Tanespimycin (17-AAG)

别名: CP127374, NSC-330507, KOS 953 中文名称:坦螺旋霉素

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂,无细胞试验中IC50为5 nM,作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。

Tanespimycin (17-AAG) Chemical Structure

Tanespimycin (17-AAG) Chemical Structure

CAS: 75747-14-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) 958.23 现货
5mg 795.18 现货
25mg 2432.97 现货
100mg 6527.43 现货
1g 30459.42 现货
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400-668-6834

info@selleck.cn

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Tanespimycin (17-AAG)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
C2BBe1 Growth Inhibition Assay IC50=0.2219 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.21786 μM SANGER
MFE-280 Growth Inhibition Assay IC50=0.21298 μM SANGER
769-P Growth Inhibition Assay IC50=0.2128 μM SANGER
HPAF-II Growth Inhibition Assay IC50=0.21264 μM SANGER
A172 Growth Inhibition Assay IC50=0.21022 μM SANGER
AM-38 Growth Inhibition Assay IC50=0.20848 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=0.20769 μM SANGER
S-117 Growth Inhibition Assay IC50=0.20564 μM SANGER
U031 Growth Inhibition Assay IC50=0.20547 μM SANGER
SBC-5 Growth Inhibition Assay IC50=0.20118 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=0.20057 μM SANGER
COLO-680N Growth Inhibition Assay IC50=0.19364 μM SANGER
Capan-2 Growth Inhibition Assay IC50=0.19256 μM SANGER
RVH-421 Growth Inhibition Assay IC50=0.19116 μM SANGER
RD Growth Inhibition Assay IC50=0.19113 μM SANGER
CAL-27 Growth Inhibition Assay IC50=0.19022 μM SANGER
BCPAP Growth Inhibition Assay IC50=0.18872 μM SANGER
JEG-3 Growth Inhibition Assay IC50=0.18705 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=0.18682 μM SANGER
DEL Growth Inhibition Assay IC50=0.1845 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.18443 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.18394 μM SANGER
LK-2 Growth Inhibition Assay IC50=0.18303 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=0.182 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=0.18082 μM SANGER
SCC-4 Growth Inhibition Assay IC50=0.17777 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=0.17734 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.17682 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.17649 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=0.17571 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=0.17536 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=0.17368 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.1733 μM SANGER
COLO-824 Growth Inhibition Assay IC50=0.17294 μM SANGER
U-2-OS Growth Inhibition Assay IC50=0.17173 μM SANGER
HT-1376 Growth Inhibition Assay IC50=0.16936 μM SANGER
SCC-9 Growth Inhibition Assay IC50=0.16716 μM SANGER
OC-314 Growth Inhibition Assay IC50=0.1669 μM SANGER
FTC-133 Growth Inhibition Assay IC50=0.1654 μM SANGER
SW1088 Growth Inhibition Assay IC50=0.16413 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=0.16285 μM SANGER
HCC1937 Growth Inhibition Assay IC50=0.16275 μM SANGER
CAL-62 Growth Inhibition Assay IC50=0.16169 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=0.15966 μM SANGER
ETK-1 Growth Inhibition Assay IC50=0.159 μM SANGER
786-0 Growth Inhibition Assay IC50=0.15381 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.15232 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=0.15225 μM SANGER
639-V Growth Inhibition Assay IC50=0.15013 μM SANGER
Mewo Growth Inhibition Assay IC50=0.14889 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=0.14839 μM SANGER
SW1573 Growth Inhibition Assay IC50=0.14758 μM SANGER
HCC1419 Growth Inhibition Assay IC50=0.14576 μM SANGER
GI-1 Growth Inhibition Assay IC50=0.14558 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=0.14478 μM SANGER
MPP-89 Growth Inhibition Assay IC50=0.14125 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.14121 μM SANGER
GP5d Growth Inhibition Assay IC50=0.14104 μM SANGER
RT-112 Growth Inhibition Assay IC50=0.14035 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=0.13956 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=0.13883 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=0.1387 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=0.13762 μM SANGER
GAK Growth Inhibition Assay IC50=0.13567 μM SANGER
BPH-1 Growth Inhibition Assay IC50=0.1341 μM SANGER
PC-14 Growth Inhibition Assay IC50=0.13211 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=0.1311 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=0.12943 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=0.12924 μM SANGER
A375 Growth Inhibition Assay IC50=0.12778 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=0.12774 μM SANGER
SAS Growth Inhibition Assay IC50=0.1269 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.12661 μM SANGER
SNB75 Growth Inhibition Assay IC50=0.12169 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=0.12157 μM SANGER
SW1990 Growth Inhibition Assay IC50=0.12157 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.1202 μM SANGER
COLO-829 Growth Inhibition Assay IC50=0.12005 μM SANGER
RXF393 Growth Inhibition Assay IC50=0.11982 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=0.11817 μM SANGER
BT-549 Growth Inhibition Assay IC50=0.11799 μM SANGER
OMC-1 Growth Inhibition Assay IC50=0.11797 μM SANGER
RKO Growth Inhibition Assay IC50=0.11764 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.11393 μM SANGER
SH-4 Growth Inhibition Assay IC50=0.11356 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=0.11321 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.11264 μM SANGER
COLO-679 Growth Inhibition Assay IC50=0.11211 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=0.10903 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=0.10873 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.10666 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.10554 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=0.10531 μM SANGER
U251 Growth Inhibition Assay IC50=0.10525 μM SANGER
SiHa Growth Inhibition Assay IC50=0.10486 μM SANGER
G-401 Growth Inhibition Assay IC50=0.10353 μM SANGER
U-87-MG Growth Inhibition Assay IC50=0.10307 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=0.1029 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=0.10286 μM SANGER
A498 Growth Inhibition Assay IC50=0.1018 μM SANGER
SN12C Growth Inhibition Assay IC50=0.10107 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.10054 μM SANGER
EFO-27 Growth Inhibition Assay IC50=0.09997 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=0.09745 μM SANGER
MCF7 Growth Inhibition Assay IC50=0.09677 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=0.09618 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.09472 μM SANGER
D-247MG Growth Inhibition Assay IC50=0.09455 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=0.09262 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.09204 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=0.0906 μM SANGER
M059J Growth Inhibition Assay IC50=0.09027 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.08728 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=0.08622 μM SANGER
HT-1080 Growth Inhibition Assay IC50=0.08439 μM SANGER
MKN45 Growth Inhibition Assay IC50=0.08219 μM SANGER
A431 Growth Inhibition Assay IC50=0.0821 μM SANGER
L-363 Growth Inhibition Assay IC50=0.08206 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=0.08043 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.07996 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=0.07969 μM SANGER
M14 Growth Inhibition Assay IC50=0.07913 μM SANGER
CAL-39 Growth Inhibition Assay IC50=0.07766 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.07589 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.07347 μM SANGER
MEL-HO Growth Inhibition Assay IC50=0.07255 μM SANGER
A2058 Growth Inhibition Assay IC50=0.07228 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=0.07208 μM SANGER
HCC1806 Growth Inhibition Assay IC50=0.07131 μM SANGER
SW620 Growth Inhibition Assay IC50=0.07026 μM SANGER
23132-87 Growth Inhibition Assay IC50=0.0695 μM SANGER
HT-29 Growth Inhibition Assay IC50=0.06919 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.06803 μM SANGER
GMS-10 Growth Inhibition Assay IC50=0.06699 μM SANGER
SF539 Growth Inhibition Assay IC50=0.06681 μM SANGER
SW684 Growth Inhibition Assay IC50=0.06591 μM SANGER
HEC-1 Growth Inhibition Assay IC50=0.06588 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=0.06553 μM SANGER
SF295 Growth Inhibition Assay IC50=0.06452 μM SANGER
KM12 Growth Inhibition Assay IC50=0.06348 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=0.06341 μM SANGER
LU-99A Growth Inhibition Assay IC50=0.06237 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=0.06205 μM SANGER
TCCSUP Growth Inhibition Assay IC50=0.05964 μM SANGER
GT3TKB Growth Inhibition Assay IC50=0.05942 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.05872 μM SANGER
5637 Growth Inhibition Assay IC50=0.0574 μM SANGER
YH-13 Growth Inhibition Assay IC50=0.05722 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=0.05414 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=0.05296 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=0.05237 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=0.05235 μM SANGER
YKG-1 Growth Inhibition Assay IC50=0.05071 μM SANGER
SW48 Growth Inhibition Assay IC50=0.05039 μM SANGER
AN3-CA Growth Inhibition Assay IC50=0.05 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=0.04986 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.04912 μM SANGER
DOK Growth Inhibition Assay IC50=0.04902 μM SANGER
G-402 Growth Inhibition Assay IC50=0.04789 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=0.04772 μM SANGER
KP-4 Growth Inhibition Assay IC50=0.04753 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=0.04649 μM SANGER
PSN1 Growth Inhibition Assay IC50=0.04603 μM SANGER
CaR-1 Growth Inhibition Assay IC50=0.04549 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.045 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=0.04475 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=0.04447 μM SANGER
H9 Growth Inhibition Assay IC50=0.04371 μM SANGER
HN Growth Inhibition Assay IC50=0.04272 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=0.04243 μM SANGER
Detroit562 Growth Inhibition Assay IC50=0.04239 μM SANGER
SW780 Growth Inhibition Assay IC50=0.04203 μM SANGER
ACN Growth Inhibition Assay IC50=0.04162 μM SANGER
T98G Growth Inhibition Assay IC50=0.04103 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=0.04021 μM SANGER
TYK-nu Growth Inhibition Assay IC50=0.03985 μM SANGER
SW962 Growth Inhibition Assay IC50=0.03945 μM SANGER
Becker Growth Inhibition Assay IC50=0.03885 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.03807 μM SANGER
WM-115 Growth Inhibition Assay IC50=0.03762 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=0.03657 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=0.03606 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=0.0348 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=0.0345 μM SANGER
GAMG Growth Inhibition Assay IC50=0.03435 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=0.03354 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.03309 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=0.03178 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.03093 μM SANGER
H4 Growth Inhibition Assay IC50=0.0309 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=0.03082 μM SANGER
OE19 Growth Inhibition Assay IC50=0.03077 μM SANGER
SW982 Growth Inhibition Assay IC50=0.02999 μM SANGER
ME-180 Growth Inhibition Assay IC50=0.02891 μM SANGER
D-263MG Growth Inhibition Assay IC50=0.02786 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=0.02665 μM SANGER
CHP-212 Growth Inhibition Assay IC50=0.02628 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=0.02593 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.02546 μM SANGER
A2780 Growth Inhibition Assay IC50=0.02531 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.02494 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.02349 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.02261 μM SANGER
CHL-1 Growth Inhibition Assay IC50=0.02251 μM SANGER
A204 Growth Inhibition Assay IC50=0.02249 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=0.01974 μM SANGER
AGS Growth Inhibition Assay IC50=0.01938 μM SANGER
TI-73 Growth Inhibition Assay IC50=0.01796 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=0.01495 μM SANGER
CAL-51 Growth Inhibition Assay IC50=0.01405 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.01355 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=0.01009 μM SANGER
HSC-3 Growth Inhibition Assay IC50=0.00929 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=0.00717 μM SANGER
HGC-27 Growth Inhibition Assay IC50=0.0051 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.00419 μM SANGER
D-566MG Growth Inhibition Assay IC50=0.0039 μM SANGER
C32 Growth Inhibition Assay IC50=0.00304 μM SANGER
FADU Growth Inhibition Assay IC50=0.00209 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=0.00207 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.000407 μM SANGER
A549 Growth Inhibition Assay IC50=0.000303 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.22203 μM SANGER
G-361 Growth Inhibition Assay IC50=0.22682 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=0.23084 μM SANGER
TK10 Growth Inhibition Assay IC50=0.23117 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.23119 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=0.23681 μM SANGER
BHY Growth Inhibition Assay IC50=0.23691 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.23961 μM SANGER
COLO-678 Growth Inhibition Assay IC50=0.24044 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.24169 μM SANGER
K5 Growth Inhibition Assay IC50=0.2438 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.24509 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=0.24529 μM SANGER
SCC-25 Growth Inhibition Assay IC50=0.24563 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=0.24783 μM SANGER
ESS-1 Growth Inhibition Assay IC50=0.24805 μM SANGER
TE-6 Growth Inhibition Assay IC50=0.2575 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.25777 μM SANGER
COLO-800 Growth Inhibition Assay IC50=0.25812 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.26136 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=0.26162 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.26363 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=0.26506 μM SANGER
HCT-116 Growth Inhibition Assay IC50=0.26599 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=0.26678 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.26742 μM SANGER
NB69 Growth Inhibition Assay IC50=0.27087 μM SANGER
J82 Growth Inhibition Assay IC50=0.27265 μM SANGER
U-118-MG Growth Inhibition Assay IC50=0.27579 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.28074 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=0.28956 μM SANGER
SW954 Growth Inhibition Assay IC50=0.29227 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.29277 μM SANGER
SW1710 Growth Inhibition Assay IC50=0.29494 μM SANGER
KY821 Growth Inhibition Assay IC50=0.29872 μM SANGER
HCC38 Growth Inhibition Assay IC50=0.30078 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=0.3054 μM SANGER
ES8 Growth Inhibition Assay IC50=0.30784 μM SANGER
COLO-792 Growth Inhibition Assay IC50=0.31251 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=0.31521 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=0.31715 μM SANGER
Daoy Growth Inhibition Assay IC50=0.31723 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=0.31847 μM SANGER
KNS-62 Growth Inhibition Assay IC50=0.32088 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=0.32111 μM SANGER
UACC-62 Growth Inhibition Assay IC50=0.32227 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=0.32283 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.32753 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.32836 μM SANGER
T-24 Growth Inhibition Assay IC50=0.33159 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=0.33283 μM SANGER
SW626 Growth Inhibition Assay IC50=0.33532 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=0.33619 μM SANGER
DMS-273 Growth Inhibition Assay IC50=0.33916 μM SANGER
SW1783 Growth Inhibition Assay IC50=0.33997 μM SANGER
KU812 Growth Inhibition Assay IC50=0.34038 μM SANGER
HSC-2 Growth Inhibition Assay IC50=0.34053 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.34162 μM SANGER
COLO-684 Growth Inhibition Assay IC50=0.34501 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=0.34631 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=0.35357 μM SANGER
NB13 Growth Inhibition Assay IC50=0.36829 μM SANGER
no-11 Growth Inhibition Assay IC50=0.3695 μM SANGER
DK-MG Growth Inhibition Assay IC50=0.37188 μM SANGER
NBsusSR Growth Inhibition Assay IC50=0.37285 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=0.37463 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=0.37518 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.37862 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=0.3851 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.38603 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=0.38703 μM SANGER
HCC2157 Growth Inhibition Assay IC50=0.38781 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.38941 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=0.39699 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=0.40143 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=0.4117 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=0.41446 μM SANGER
TE-10 Growth Inhibition Assay IC50=0.41447 μM SANGER
HOS Growth Inhibition Assay IC50=0.41682 μM SANGER
LN-405 Growth Inhibition Assay IC50=0.41687 μM SANGER
A427 Growth Inhibition Assay IC50=0.41981 μM SANGER
CAL-12T Growth Inhibition Assay IC50=0.4278 μM SANGER
SW756 Growth Inhibition Assay IC50=0.44183 μM SANGER
YAPC Growth Inhibition Assay IC50=0.4508 μM SANGER
GOTO Growth Inhibition Assay IC50=0.4516 μM SANGER
C3A Growth Inhibition Assay IC50=0.45437 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=0.4547 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=0.45569 μM SANGER
LS-411N Growth Inhibition Assay IC50=0.46527 μM SANGER
COR-L23 Growth Inhibition Assay IC50=0.46764 μM SANGER
HCE-4 Growth Inhibition Assay IC50=0.47446 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=0.47896 μM SANGER
A101D Growth Inhibition Assay IC50=0.48053 μM SANGER
HT-3 Growth Inhibition Assay IC50=0.48217 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.49865 μM SANGER
PC-3 Growth Inhibition Assay IC50=0.51507 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.52669 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=0.53177 μM SANGER
CAL-120 Growth Inhibition Assay IC50=0.53399 μM SANGER
UMC-11 Growth Inhibition Assay IC50=0.55234 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=0.55762 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=0.56815 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=0.57977 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=0.58053 μM SANGER
MKN1 Growth Inhibition Assay IC50=0.58783 μM SANGER
ES3 Growth Inhibition Assay IC50=0.59124 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=0.59341 μM SANGER
ACHN Growth Inhibition Assay IC50=0.60569 μM SANGER
SW872 Growth Inhibition Assay IC50=0.60763 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=0.60969 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=0.61104 μM SANGER
UACC-893 Growth Inhibition Assay IC50=0.63681 μM SANGER
JVM-3 Growth Inhibition Assay IC50=0.63804 μM SANGER
SF268 Growth Inhibition Assay IC50=0.64349 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=0.65397 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.66323 μM SANGER
MKN28 Growth Inhibition Assay IC50=0.66624 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=0.6718 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.68679 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.68726 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=0.7 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=0.70829 μM SANGER
8305C Growth Inhibition Assay IC50=0.72498 μM SANGER
EFM-19 Growth Inhibition Assay IC50=0.73671 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=0.74613 μM SANGER
A388 Growth Inhibition Assay IC50=0.76467 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.77235 μM SANGER
IGR-1 Growth Inhibition Assay IC50=0.79043 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=0.80004 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=0.81508 μM SANGER
UACC-257 Growth Inhibition Assay IC50=0.82231 μM SANGER
OE33 Growth Inhibition Assay IC50=0.85101 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.85141 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=0.85311 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=0.87783 μM SANGER
Saos-2 Growth Inhibition Assay IC50=0.87871 μM SANGER
NB17 Growth Inhibition Assay IC50=0.88025 μM SANGER
D-392MG Growth Inhibition Assay IC50=0.89356 μM SANGER
SHP-77 Growth Inhibition Assay IC50=0.90485 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=0.91185 μM SANGER
GCIY Growth Inhibition Assay IC50=0.91843 μM SANGER
HCC70 Growth Inhibition Assay IC50=0.92059 μM SANGER
LU-65 Growth Inhibition Assay IC50=0.92591 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=0.94865 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=0.95192 μM SANGER
PA-1 Growth Inhibition Assay IC50=0.95424 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.97489 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.97634 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=0.98626 μM SANGER
8505C Growth Inhibition Assay IC50=0.99982 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.00084 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=1.01428 μM SANGER
EKVX Growth Inhibition Assay IC50=1.03121 μM SANGER
RCM-1 Growth Inhibition Assay IC50=1.05507 μM SANGER
SW900 Growth Inhibition Assay IC50=1.0783 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.07855 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=1.10056 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=1.10154 μM SANGER
SW837 Growth Inhibition Assay IC50=1.10954 μM SANGER
BT-20 Growth Inhibition Assay IC50=1.11204 μM SANGER
RH-18 Growth Inhibition Assay IC50=1.13103 μM SANGER
TE-12 Growth Inhibition Assay IC50=1.13333 μM SANGER
NB10 Growth Inhibition Assay IC50=1.13344 μM SANGER
AU565 Growth Inhibition Assay IC50=1.15973 μM SANGER
OAW-42 Growth Inhibition Assay IC50=1.18306 μM SANGER
DJM-1 Growth Inhibition Assay IC50=1.19881 μM SANGER
HH Growth Inhibition Assay IC50=1.23831 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=1.27394 μM SANGER
KNS-42 Growth Inhibition Assay IC50=1.30296 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=1.30507 μM SANGER
MLMA Growth Inhibition Assay IC50=1.32407 μM SANGER
NB12 Growth Inhibition Assay IC50=1.35636 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=1.36306 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=1.37853 μM SANGER
LS-123 Growth Inhibition Assay IC50=1.39094 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=1.39271 μM SANGER
MC-IXC Growth Inhibition Assay IC50=1.42371 μM SANGER
HCT-15 Growth Inhibition Assay IC50=1.43068 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=1.45061 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=1.47082 μM SANGER
A704 Growth Inhibition Assay IC50=1.66563 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=1.69607 μM SANGER
SW1417 Growth Inhibition Assay IC50=1.72849 μM SANGER
CAS-1 Growth Inhibition Assay IC50=1.73936 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=1.79759 μM SANGER
A253 Growth Inhibition Assay IC50=1.82239 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.82875 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.86988 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=1.89359 μM SANGER
HOP-92 Growth Inhibition Assay IC50=1.96099 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=2.02337 μM SANGER
LU-139 Growth Inhibition Assay IC50=2.03114 μM SANGER
SJRH30 Growth Inhibition Assay IC50=2.04253 μM SANGER
MG-63 Growth Inhibition Assay IC50=2.14111 μM SANGER
NH-12 Growth Inhibition Assay IC50=2.15006 μM SANGER
NB7 Growth Inhibition Assay IC50=2.19673 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=2.20595 μM SANGER
HCC1569 Growth Inhibition Assay IC50=2.24583 μM SANGER
D-283MED Growth Inhibition Assay IC50=2.24782 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=2.25351 μM SANGER
ATN-1 Growth Inhibition Assay IC50=2.33082 μM SANGER
HCC1954 Growth Inhibition Assay IC50=2.34408 μM SANGER
SCC-15 Growth Inhibition Assay IC50=2.39312 μM SANGER
COLO-668 Growth Inhibition Assay IC50=2.432 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=2.54677 μM SANGER
no-10 Growth Inhibition Assay IC50=2.54947 μM SANGER
HT-1197 Growth Inhibition Assay IC50=2.63188 μM SANGER
DU-145 Growth Inhibition Assay IC50=2.79162 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=2.84692 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=2.85322 μM SANGER
EW-22 Growth Inhibition Assay IC50=2.92841 μM SANGER
DB Growth Inhibition Assay IC50=2.97759 μM SANGER
HL-60 Growth Inhibition Assay IC50=3.04376 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=3.05075 μM SANGER
NY Growth Inhibition Assay IC50=3.08542 μM SANGER
T47D Growth Inhibition Assay IC50=3.10558 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=3.22477 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=3.26027 μM SANGER
KM-H2 Growth Inhibition Assay IC50=3.3068 μM SANGER
CHP-134 Growth Inhibition Assay IC50=3.4739 μM SANGER
22RV1 Growth Inhibition Assay IC50=3.49168 μM SANGER
NB5 Growth Inhibition Assay IC50=3.50689 μM SANGER
CW-2 Growth Inhibition Assay IC50=3.55314 μM SANGER
EFO-21 Growth Inhibition Assay IC50=3.5694 μM SANGER
HuH-7 Growth Inhibition Assay IC50=3.58414 μM SANGER
ALL-PO Growth Inhibition Assay IC50=3.62335 μM SANGER
EM-2 Growth Inhibition Assay IC50=3.69011 μM SANGER
KLE Growth Inhibition Assay IC50=3.73029 μM SANGER
NEC8 Growth Inhibition Assay IC50=3.91808 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=3.93476 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=4.03518 μM SANGER
CAL-54 Growth Inhibition Assay IC50=4.0591 μM SANGER
MS-1 Growth Inhibition Assay IC50=4.16155 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=4.29999 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=4.32131 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=4.36327 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=4.39736 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=4.45691 μM SANGER
ES4 Growth Inhibition Assay IC50=4.47095 μM SANGER
ES6 Growth Inhibition Assay IC50=4.49657 μM SANGER
DMS-114 Growth Inhibition Assay IC50=4.54691 μM SANGER
ONS-76 Growth Inhibition Assay IC50=4.5795 μM SANGER
K-562 Growth Inhibition Assay IC50=4.73814 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=4.75461 μM SANGER
Calu-3 Growth Inhibition Assay IC50=4.78548 μM SANGER
HT55 Growth Inhibition Assay IC50=4.84545 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=4.85009 μM SANGER
ES1 Growth Inhibition Assay IC50=4.86057 μM SANGER
SF126 Growth Inhibition Assay IC50=4.93184 μM SANGER
ES5 Growth Inhibition Assay IC50=5.12427 μM SANGER
LoVo Growth Inhibition Assay IC50=5.15871 μM SANGER
SNU-387 Growth Inhibition Assay IC50=5.32339 μM SANGER
C8166 Growth Inhibition Assay IC50=5.36339 μM SANGER
LS-1034 Growth Inhibition Assay IC50=5.42307 μM SANGER
GR-ST Growth Inhibition Assay IC50=5.52201 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=5.72843 μM SANGER
647-V Growth Inhibition Assay IC50=5.74706 μM SANGER
EW-13 Growth Inhibition Assay IC50=5.76627 μM SANGER
KGN Growth Inhibition Assay IC50=6.09921 μM SANGER
D-423MG Growth Inhibition Assay IC50=6.40284 μM SANGER
ECC10 Growth Inhibition Assay IC50=7.10101 μM SANGER
TE-5 Growth Inhibition Assay IC50=7.41298 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=7.45523 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=7.45701 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=7.83063 μM SANGER
RH-1 Growth Inhibition Assay IC50=7.85244 μM SANGER
SW948 Growth Inhibition Assay IC50=7.96049 μM SANGER
CAL-33 Growth Inhibition Assay IC50=7.99938 μM SANGER
U-266 Growth Inhibition Assay IC50=8.15777 μM SANGER
CAL-72 Growth Inhibition Assay IC50=8.2032 μM SANGER
SNU-423 Growth Inhibition Assay IC50=9.36666 μM SANGER
KG-1 Growth Inhibition Assay IC50=9.58456 μM SANGER
HCC1395 Growth Inhibition Assay IC50=9.92352 μM SANGER
BE-13 Growth Inhibition Assay IC50=10.8892 μM SANGER
MKN7 Growth Inhibition Assay IC50=10.9765 μM SANGER
697 Growth Inhibition Assay IC50=11.1472 μM SANGER
LU-135 Growth Inhibition Assay IC50=11.2307 μM SANGER
ES7 Growth Inhibition Assay IC50=11.3313 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=11.7646 μM SANGER
BEN Growth Inhibition Assay IC50=11.851 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=12.126 μM SANGER
SW13 Growth Inhibition Assay IC50=12.1541 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=12.5452 μM SANGER
Mo-T Growth Inhibition Assay IC50=12.7421 μM SANGER
HLE Growth Inhibition Assay IC50=12.8215 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=13.671 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=13.7381 μM SANGER
BHT-101 Growth Inhibition Assay IC50=13.8345 μM SANGER
OCUB-M Growth Inhibition Assay IC50=14.1602 μM SANGER
MEG-01 Growth Inhibition Assay IC50=14.3708 μM SANGER
RS4-11 Growth Inhibition Assay IC50=14.742 μM SANGER
MN-60 Growth Inhibition Assay IC50=14.7894 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=15.0425 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=15.0581 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=15.2044 μM SANGER
LAN-6 Growth Inhibition Assay IC50=15.4414 μM SANGER
JVM-2 Growth Inhibition Assay IC50=15.5748 μM SANGER
P30-OHK Growth Inhibition Assay IC50=16.0614 μM SANGER
C-33-A Growth Inhibition Assay IC50=16.6214 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=16.8496 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=16.8537 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=17.2028 μM SANGER
T84 Growth Inhibition Assay IC50=18.8695 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=18.9608 μM SANGER
BALL-1 Growth Inhibition Assay IC50=19.3399 μM SANGER
Calu-6 Growth Inhibition Assay IC50=19.492 μM SANGER
EGI-1 Growth Inhibition Assay IC50=19.598 μM SANGER
MFH-ino Growth Inhibition Assay IC50=19.7454 μM SANGER
GB-1 Growth Inhibition Assay IC50=20.3535 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=20.6505 μM SANGER
SW1116 Growth Inhibition Assay IC50=20.9362 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=22.045 μM SANGER
D-502MG Growth Inhibition Assay IC50=22.8261 μM SANGER
IA-LM Growth Inhibition Assay IC50=23.2493 μM SANGER
SW1463 Growth Inhibition Assay IC50=23.79 μM SANGER
JAR Growth Inhibition Assay IC50=24.3293 μM SANGER
HT Growth Inhibition Assay IC50=24.4753 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=24.8449 μM SANGER
SNU-449 Growth Inhibition Assay IC50=24.8741 μM SANGER
KE-37 Growth Inhibition Assay IC50=25.0928 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=27.1303 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=27.3516 μM SANGER
COLO-741 Growth Inhibition Assay IC50=31.3333 μM SANGER
NB6 Growth Inhibition Assay IC50=32.2876 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=33.0055 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=34.0541 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=35.066 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=35.2817 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=37.1536 μM SANGER
HAL-01 Growth Inhibition Assay IC50=38.4889 μM SANGER
HEL Growth Inhibition Assay IC50=43.3409 μM SANGER
EW-1 Growth Inhibition Assay IC50=43.4768 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=45.1199 μM SANGER
ABC-1 Growth Inhibition Assay IC50=46.8538 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=48.5058 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=49.6007 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=49.6656 μM SANGER
GCT Growth Inhibition Assay IC50=49.6976 μM SANGER
点击查看更多细胞系数据

生物活性

产品描述 Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂,无细胞试验中IC50为5 nM,作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。
特性 17-AAG对正常细胞的毒性很小。
靶点
HSP90 [1]
(Cell-free assay)
5 nM
体外研究(In Vitro)
体外研究活性

17-AAG是格尔德霉素类似物, 但是与过量表达HER-2的癌细胞 (BT474, N87, SKOV3 和SKBR3)或BT474乳腺细胞衍生的Hsp90亲和力高100多倍,IC50为5-6 nM, 而作用于正常人类原代细胞时,IC50为400-943 nM, 因为肿瘤Hsp90 处于多伴复合体状态,具有高ATP酶活性,而正常细胞Hsp90 处于潜在未结合状态, 且直接与那些细胞中17-AAG毒性相关。[1]17-AAG 引起HER2, HER3, Akt,突变和野生型雄激素受体(AR)降解,导致前列腺细胞如LNCaP, LAPC-4, DU-145,和PC-3中RB依赖的 G1 期生长停顿,IC50为25-45 nM。[2]除了诱导改变野生型BCR-ABL的Ba/F3细胞凋亡, IC50为5.2 μM, 17-AAG还通过诱导野生型和突变型 BCR-ABL蛋白降解,而诱导改变T315I和 E255K BCR-ABL突变型细胞生长,IC50分别为2.3 μM 和 1.0 μM。[3]

激酶实验 Hsp90结合实验
纯化的Hsp90蛋白或过量表达HER-2的癌细胞(BT474, N87, SKOV3 和 SKBR3) 裂解物或BT474乳腺癌细胞溶于溶解buffer(20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) ,与不同浓度17-AAG在4oC下温育30分钟,然后和生物素-GM链接的BioMag链霉亲和素磁珠在4oC下温育1小时。试管放置于磁架上,除去未结合的上清液。在溶解buffer中清洗三次磁珠,然后在SDS–PAGE 样本缓冲液中在95oC下加热5分钟。在SDS蛋白凝胶上进行样本分析,使用特点抗体进行Western Blotting。使用Bio-rad Fluor-S 多重图像测量Western Blot条带,计算抑制Hsp90与生物素-GM结合的百分数。测定IC50。
细胞实验 细胞系 BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, 和 PBMC
浓度 溶于DMSO, 终浓度为10 μM 左右
孵育时间 5天
方法

细胞按每孔2000个接种在96孔板上,终培养体积为100 μL,培养24小时, 然后加入浓度不断增高的17-AAG,温育5天。使用 Celltiter 96 AQueous 非放射性细胞增殖检测试剂盒测定存活细胞数。测定IC50。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin EGFR / PDGFR / AKT / MAPK / c-RAS pAKT / pMAPK / pRb Cleaved PARP / Survivin LATS1 / p-LATS1 / YAP / CTGF 20090920
Immunofluorescence STAT3 YAP / TAZ β-catenin / E-cadherin 27279418
Growth inhibition assay Cell viability 18682579
体内研究(In Vivo)
体内研究活性

17-AAG作用于携带3T3-src, B16或CT26移植瘤裸鼠,与Hsp90结合具有高亲和力,IC50为8-35 nM,而作用于正常组织时,IC50为200-600 nM。[1] 17-AAG按50 mg/kg左右剂量处理,引起AR, HER2, HER3, 和 Akt表达明显降低,降低达50%以上,这种作用存在剂量依赖性,结果导致雄激素依赖型 (CWR22)和非依赖型(CWR22R 和CWRSA6) 前列腺移植瘤生长受抑制,抑制率分别为67%, 80%和 68%。[2]

动物实验 Animal Models 皮下注射雄激素依赖性CWR22移植瘤的雄性 nu/nu 无胸腺小鼠, 皮下注射雄激素非依赖性的CWR22R和CWRSA6移植瘤的雌性nu/nu 无胸腺小鼠。
Dosages 50 mg/kg 左右
Administration 腹膜注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00103272 Terminated
Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia
National Cancer Institute (NCI)
April 2005 Phase 1
NCT00098488 Terminated
B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia
National Cancer Institute (NCI)
April 2005 Phase 1
NCT00118248 Completed
Recurrent Thyroid Cancer|Stage IV Follicular Thyroid Cancer|Stage IV Papillary Thyroid Cancer|Thyroid Gland Medullary Carcinoma
National Cancer Institute (NCI)
December 2004 Phase 2
NCT00098423 Completed
Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts in Transformation|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes
National Cancer Institute (NCI)
November 2004 Phase 1

化学信息&溶解度

分子量 585.69 分子式

C31H43N3O8

CAS号 75747-14-7 SDF Download Tanespimycin (17-AAG) SDF
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (170.73 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 33 mg/mL (56.34 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
What kind of subtypes does this compound inhibit? HSP90α or HSP90β ?

回答:
17-AAG can inhibit both HSP90α and HSP90β, but it is unclear how much are they affected respectively. You should note that Hsp90 derived from tumor cells has a 100-fold higher binding affinity for 17-AAG than that from normal cells according to this paper. http://www.nature.com.ezp-prod1.hul.harvard.edu/nature/journal/v425/n6956/full/nature01913.html

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