Home Protein Tyrosine Kinase ALK inhibitor - Apoptosis related activator TAE684 (NVP-TAE684) 仅限科研使用

TAE684 (NVP-TAE684)

TAE684 (NVP-TAE684) 是一种有效的，选择性 ALK 抑制剂，能阻断ALCL来源的ALK依赖性细胞系的生长，IC50 介于2nM到10nM之间，作用于ALK比作用于InsR选择性高100倍。TAE684 (NVP-TAE684) 可诱导细胞周期阻滞和凋亡。

TAE684 (NVP-TAE684) Chemical Structure

TAE684 (NVP-TAE684) Chemical Structure

CAS: 761439-42-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 2201.25 现货
5mg 1308.07 现货
10mg 2379.43 现货
50mg 6308.29 现货
200mg 15315.3 现货
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TAE684 (NVP-TAE684)相关产品

相关信号通路图

ALK Signaling Pathways

ALK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(PMID)
SCC-3 Growth Inhibition Assay IC50=0.0000603 μM
SF539 Growth Inhibition Assay IC50=0.000564 μM
DEL Growth Inhibition Assay IC50=0.000927 μM
NB1 Growth Inhibition Assay IC50=0.00162 μM
SR Growth Inhibition Assay IC50=0.00277 μM
KARPAS-299 Growth Inhibition Assay IC50=0.02384 μM
MHH-CALL-2 Growth Inhibition Assay IC50=0.02952 μM
SU-DHL-1 Growth Inhibition Assay IC50=0.04865 μM
A4-Fuk Growth Inhibition Assay IC50=0.05565 μM
EW-1 Growth Inhibition Assay IC50=0.10256 μM
NOS-1 Growth Inhibition Assay IC50=0.10294 μM
EW-16 Growth Inhibition Assay IC50=0.10568 μM
TE-11 Growth Inhibition Assay IC50=0.16096 μM
SW982 Growth Inhibition Assay IC50=0.16478 μM
LAN-6 Growth Inhibition Assay IC50=0.17443 μM
MZ1-PC Growth Inhibition Assay IC50=0.17835 μM
KS-1 Growth Inhibition Assay IC50=0.19343 μM
PSN1 Growth Inhibition Assay IC50=0.19631 μM
LC-2-ad Growth Inhibition Assay IC50=0.19692 μM
COLO-320-HSR Growth Inhibition Assay IC50=0.19776 μM
OPM-2 Growth Inhibition Assay IC50=0.22669 μM
SK-NEP-1 Growth Inhibition Assay IC50=0.23524 μM
ALL-PO Growth Inhibition Assay IC50=0.24524 μM
CMK Growth Inhibition Assay IC50=0.2553 μM
NCI-H1648 Growth Inhibition Assay IC50=0.27855 μM
SIG-M5 Growth Inhibition Assay IC50=0.29159 μM
TGBC24TKB Growth Inhibition Assay IC50=0.30218 μM
DOHH-2 Growth Inhibition Assay IC50=0.31204 μM
NB69 Growth Inhibition Assay IC50=0.31787 μM
MFH-ino Growth Inhibition Assay IC50=0.32523 μM
KP-N-RT-BM-1 Growth Inhibition Assay IC50=0.33123 μM
MONO-MAC-6 Growth Inhibition Assay IC50=0.33291 μM
ATN-1 Growth Inhibition Assay IC50=0.33303 μM
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.33396 μM
L-540 Growth Inhibition Assay IC50=0.36988 μM
GB-1 Growth Inhibition Assay IC50=0.38867 μM
MV-4-11 Growth Inhibition Assay IC50=0.39446 μM
KG-1 Growth Inhibition Assay IC50=0.39561 μM
OVCAR-4 Growth Inhibition Assay IC50=0.40569 μM
NEC8 Growth Inhibition Assay IC50=0.41292 μM
SK-MM-2 Growth Inhibition Assay IC50=0.41609 μM
TE-8 Growth Inhibition Assay IC50=0.4288 μM
697 Growth Inhibition Assay IC50=0.43215 μM
NB14 Growth Inhibition Assay IC50=0.43826 μM
GDM-1 Growth Inhibition Assay IC50=0.47116 μM
HUTU-80 Growth Inhibition Assay IC50=0.47375 μM
HL-60 Growth Inhibition Assay IC50=0.48142 μM
OCI-AML2 Growth Inhibition Assay IC50=0.48328 μM
ML-2 Growth Inhibition Assay IC50=0.49031 μM
ES4 Growth Inhibition Assay IC50=0.49109 μM
NCI-H747 Growth Inhibition Assay IC50=0.4989 μM
RL95-2 Growth Inhibition Assay IC50=0.50112 μM
TE-15 Growth Inhibition Assay IC50=0.51124 μM
TE-12 Growth Inhibition Assay IC50=0.53349 μM
LB1047-RCC Growth Inhibition Assay IC50=0.54549 μM
LB831-BLC Growth Inhibition Assay IC50=0.55023 μM
NCI-H1355 Growth Inhibition Assay IC50=0.55184 μM
CTV-1 Growth Inhibition Assay IC50=0.55624 μM
RXF393 Growth Inhibition Assay IC50=0.55794 μM
SW872 Growth Inhibition Assay IC50=0.56724 μM
MPP-89 Growth Inhibition Assay IC50=0.57884 μM
RPMI-8226 Growth Inhibition Assay IC50=0.63526 μM
LS-1034 Growth Inhibition Assay IC50=0.6358 μM
SJSA-1 Growth Inhibition Assay IC50=0.63725 μM
HOP-62 Growth Inhibition Assay IC50=0.65033 μM
KGN Growth Inhibition Assay IC50=0.66168 μM
D-336MG Growth Inhibition Assay IC50=0.66169 μM
LS-411N Growth Inhibition Assay IC50=0.67462 μM
TE-1 Growth Inhibition Assay IC50=0.69074 μM
LB996-RCC Growth Inhibition Assay IC50=0.69389 μM
TE-10 Growth Inhibition Assay IC50=0.71496 μM
NCI-SNU-16 Growth Inhibition Assay IC50=0.72664 μM
ES8 Growth Inhibition Assay IC50=0.74975 μM
COLO-800 Growth Inhibition Assay IC50=0.76695 μM
ES6 Growth Inhibition Assay IC50=0.77559 μM
L-363 Growth Inhibition Assay IC50=0.82375 μM
NMC-G1 Growth Inhibition Assay IC50=0.83233 μM
LU-134-A Growth Inhibition Assay IC50=0.83912 μM
SF268 Growth Inhibition Assay IC50=0.84042 μM
KARPAS-45 Growth Inhibition Assay IC50=0.84263 μM
TGW Growth Inhibition Assay IC50=0.85863 μM
CHP-126 Growth Inhibition Assay IC50=0.85957 μM
MOLT-16 Growth Inhibition Assay IC50=0.87589 μM
LB771-HNC Growth Inhibition Assay IC50=0.89757 μM
NALM-6 Growth Inhibition Assay IC50=0.90739 μM
GCIY Growth Inhibition Assay IC50=0.95526 μM
IST-MES1 Growth Inhibition Assay IC50=0.98824 μM
LB2241-RCC Growth Inhibition Assay IC50=0.9884 μM
BL-70 Growth Inhibition Assay IC50=0.99535 μM
NB17 Growth Inhibition Assay IC50=1.00639 μM
LXF-289 Growth Inhibition Assay IC50=1.03076 μM
TK10 Growth Inhibition Assay IC50=1.05063 μM
K5 Growth Inhibition Assay IC50=1.06274 μM
NCI-H716 Growth Inhibition Assay IC50=1.07259 μM
HCE-T Growth Inhibition Assay IC50=1.08819 μM
GI-1 Growth Inhibition Assay IC50=1.09798 μM
KARPAS-422 Growth Inhibition Assay IC50=1.10022 μM
TE-9 Growth Inhibition Assay IC50=1.11328 μM
SF126 Growth Inhibition Assay IC50=1.11568 μM
BB30-HNC Growth Inhibition Assay IC50=1.13112 μM
NCI-H1304 Growth Inhibition Assay IC50=1.13338 μM
HEL Growth Inhibition Assay IC50=1.14895 μM
HAL-01 Growth Inhibition Assay IC50=1.15283 μM
SK-LMS-1 Growth Inhibition Assay IC50=1.15974 μM
SW954 Growth Inhibition Assay IC50=1.19567 μM
D-283MED Growth Inhibition Assay IC50=1.22379 μM
NCI-H1882 Growth Inhibition Assay IC50=1.2389 μM
GI-ME-N Growth Inhibition Assay IC50=1.25208 μM
SK-PN-DW Growth Inhibition Assay IC50=1.26348 μM
C2BBe1 Growth Inhibition Assay IC50=1.29117 μM
A704 Growth Inhibition Assay IC50=1.32689 μM
KALS-1 Growth Inhibition Assay IC50=1.3408 μM
ETK-1 Growth Inhibition Assay IC50=1.34489 μM
LB647-SCLC Growth Inhibition Assay IC50=1.34986 μM
OCUB-M Growth Inhibition Assay IC50=1.36143 μM
NCI-H720 Growth Inhibition Assay IC50=1.36378 μM
NB13 Growth Inhibition Assay IC50=1.37293 μM
GR-ST Growth Inhibition Assay IC50=1.38757 μM
DU-4475 Growth Inhibition Assay IC50=1.45853 μM
HCC2157 Growth Inhibition Assay IC50=1.46659 μM
RKO Growth Inhibition Assay IC50=1.49922 μM
LS-123 Growth Inhibition Assay IC50=1.51594 μM
NCI-H69 Growth Inhibition Assay IC50=1.55811 μM
SW962 Growth Inhibition Assay IC50=1.5613 μM
PF-382 Growth Inhibition Assay IC50=1.5696 μM
A101D Growth Inhibition Assay IC50=1.57113 μM
NB10 Growth Inhibition Assay IC50=1.57392 μM
NB5 Growth Inhibition Assay IC50=1.58476 μM
HCE-4 Growth Inhibition Assay IC50=1.6085 μM
HT-144 Growth Inhibition Assay IC50=1.6319 μM
NCI-H524 Growth Inhibition Assay IC50=1.64307 μM
NKM-1 Growth Inhibition Assay IC50=1.6866 μM
KURAMOCHI Growth Inhibition Assay IC50=1.69573 μM
NCI-H187 Growth Inhibition Assay IC50=1.70036 μM
U-266 Growth Inhibition Assay IC50=1.73842 μM
BL-41 Growth Inhibition Assay IC50=1.76272 μM
SK-N-DZ Growth Inhibition Assay IC50=1.78309 μM
Daudi Growth Inhibition Assay IC50=1.78967 μM
CPC-N Growth Inhibition Assay IC50=1.85096 μM
EM-2 Growth Inhibition Assay IC50=1.851 μM
HCC1187 Growth Inhibition Assay IC50=1.86241 μM
LP-1 Growth Inhibition Assay IC50=1.87143 μM
CAS-1 Growth Inhibition Assay IC50=1.98299 μM
NB7 Growth Inhibition Assay IC50=2.00555 μM
VA-ES-BJ Growth Inhibition Assay IC50=2.01513 μM
SNU-C2B Growth Inhibition Assay IC50=2.03351 μM
LOXIMVI Growth Inhibition Assay IC50=2.06786 μM
NCI-H1581 Growth Inhibition Assay IC50=2.11559 μM
IST-SL2 Growth Inhibition Assay IC50=2.12445 μM
NOMO-1 Growth Inhibition Assay IC50=2.17683 μM
TE-6 Growth Inhibition Assay IC50=2.1905 μM
NCI-H526 Growth Inhibition Assay IC50=2.19141 μM
MSTO-211H Growth Inhibition Assay IC50=2.20041 μM
LS-513 Growth Inhibition Assay IC50=2.22269 μM
NCI-SNU-1 Growth Inhibition Assay IC50=2.33256 μM
BB65-RCC Growth Inhibition Assay IC50=2.37493 μM
GT3TKB Growth Inhibition Assay IC50=2.39972 μM
OS-RC-2 Growth Inhibition Assay IC50=2.42341 μM
NCI-H2126 Growth Inhibition Assay IC50=2.43674 μM
SK-UT-1 Growth Inhibition Assay IC50=2.47467 μM
DMS-114 Growth Inhibition Assay IC50=2.61524 μM
ONS-76 Growth Inhibition Assay IC50=2.63641 μM
8-MG-BA Growth Inhibition Assay IC50=2.65414 μM
BOKU Growth Inhibition Assay IC50=2.72764 μM
LAMA-84 Growth Inhibition Assay IC50=2.79912 μM
ES1 Growth Inhibition Assay IC50=2.81804 μM
NCI-H1395 Growth Inhibition Assay IC50=2.82012 μM
A388 Growth Inhibition Assay IC50=2.9617 μM
NCCIT Growth Inhibition Assay IC50=3.08862 μM
HD-MY-Z Growth Inhibition Assay IC50=3.13203 μM
NCI-H510A Growth Inhibition Assay IC50=3.18943 μM
NCI-N87 Growth Inhibition Assay IC50=3.2002 μM
SCLC-21H Growth Inhibition Assay IC50=3.26859 μM
SH-4 Growth Inhibition Assay IC50=3.28797 μM
QIMR-WIL Growth Inhibition Assay IC50=3.32849 μM
KM12 Growth Inhibition Assay IC50=3.33544 μM
ST486 Growth Inhibition Assay IC50=3.53883 μM
HC-1 Growth Inhibition Assay IC50=3.62028 μM
BV-173 Growth Inhibition Assay IC50=3.64088 μM
EW-24 Growth Inhibition Assay IC50=3.66434 μM
LU-65 Growth Inhibition Assay IC50=3.6871 μM
ECC4 Growth Inhibition Assay IC50=3.7756 μM
ARH-77 Growth Inhibition Assay IC50=4.11067 μM
BC-3 Growth Inhibition Assay IC50=4.13068 μM
SNB75 Growth Inhibition Assay IC50=4.2619 μM
MEG-01 Growth Inhibition Assay IC50=4.27419 μM
NCI-H1417 Growth Inhibition Assay IC50=4.28443 μM
MDA-MB-134-VI Growth Inhibition Assay IC50=4.30601 μM
Becker Growth Inhibition Assay IC50=4.47336 μM
DMS-153 Growth Inhibition Assay IC50=4.66475 μM
TGBC1TKB Growth Inhibition Assay IC50=4.68515 μM
EW-3 Growth Inhibition Assay IC50=4.76248 μM
KE-37 Growth Inhibition Assay IC50=4.86196 μM
NCI-H23 Growth Inhibition Assay IC50=4.87227 μM
MC116 Growth Inhibition Assay IC50=4.94126 μM
NH-12 Growth Inhibition Assay IC50=4.96439 μM
CTB-1 Growth Inhibition Assay IC50=4.97721 μM
KM-H2 Growth Inhibition Assay IC50=5.05323 μM
MOLT-4 Growth Inhibition Assay IC50=5.1183 μM
NCI-H2141 Growth Inhibition Assay IC50=5.14268 μM
EB-3 Growth Inhibition Assay IC50=5.17504 μM
NCI-H1522 Growth Inhibition Assay IC50=5.26322 μM
MRK-nu-1 Growth Inhibition Assay IC50=5.43633 μM
no-11 Growth Inhibition Assay IC50=5.47087 μM
CESS Growth Inhibition Assay IC50=5.58034 μM
KMOE-2 Growth Inhibition Assay IC50=5.58659 μM
REH Growth Inhibition Assay IC50=6.25618 μM
KU812 Growth Inhibition Assay IC50=6.42791 μM
SK-N-FI Growth Inhibition Assay IC50=6.60674 μM
MMAC-SF Growth Inhibition Assay IC50=7.06492 μM
RCC10RGB Growth Inhibition Assay IC50=7.22977 μM
NCI-H322M Growth Inhibition Assay IC50=7.33335 μM
NB6 Growth Inhibition Assay IC50=7.54899 μM
MN-60 Growth Inhibition Assay IC50=7.69215 μM
NCI-H1092 Growth Inhibition Assay IC50=8.01734 μM
EKVX Growth Inhibition Assay IC50=8.47066 μM
D-263MG Growth Inhibition Assay IC50=8.55396 μM
NCI-H209 Growth Inhibition Assay IC50=8.64006 μM
IST-SL1 Growth Inhibition Assay IC50=8.89892 μM
ACN Growth Inhibition Assay IC50=9.19157 μM
MHH-PREB-1 Growth Inhibition Assay IC50=9.21219 μM
EW-11 Growth Inhibition Assay IC50=9.65396 μM
KASUMI-1 Growth Inhibition Assay IC50=9.7877 μM
KINGS-1 Growth Inhibition Assay IC50=10.2347 μM
EVSA-T Growth Inhibition Assay IC50=10.3192 μM
DSH1 Growth Inhibition Assay IC50=10.3972 μM
COLO-824 Growth Inhibition Assay IC50=10.8669 μM
K052 Growth Inhibition Assay IC50=10.9322 μM
SK-MEL-2 Growth Inhibition Assay IC50=10.9939 μM
点击查看更多细胞系数据

生物活性

产品描述 TAE684 (NVP-TAE684) 是一种有效的，选择性 ALK 抑制剂，能阻断ALCL来源的ALK依赖性细胞系的生长，IC50 介于2nM到10nM之间，作用于ALK比作用于InsR选择性高100倍。TAE684 (NVP-TAE684) 可诱导细胞周期阻滞和凋亡。
特性 NVP-TAE684 作为治疗难治愈和复发的ALK阳性淋巴癌的一种策略，但是还没进行临床实验。
靶点
ALK [1]
(Cell lines)
2-10 nM
体外研究(In Vitro)
体外研究活性

NVP-TAE684选择性有效抑制ALK激酶，作用于其他激酶则没有明显的交叉反应。NVP-TAE684 有效抑制Ba/F3 NPM-ALK 细胞增殖，IC50 为3 nM, 1 μM NVP-TAE684对Ba/F3 细胞存活没有效果。NVP-TAE684 也抑制表达NPM-ALK人类ALCL细胞系的增殖，包括Karpas-299和SU-DHL-1，IC50为2-5 nM。分子模型显示L258 可能为NVP-TAE684的主要激酶选择性影响因素之一。用NVP-TAE684处理，快速且持久地抑制NPM-ALK的磷酸化作用。NVP-TAE684 作用于表达NPM-ALK的 Ba/F3 细胞和ALCL病患细胞系，诱导细胞凋亡，且使细胞周期停在G1期。[1] NVP-TAE684 作用于H3122 CR细胞，显著克服细胞特性, 含有融合致癌基因EML4-ALK, 降低细胞生长，抑制ALK磷酸化作用和诱导细胞凋亡。[2] 30 nM NVP-TAE684可抑制mALK R1279Q 突变表达诱导的神经突增生。[3]
激酶实验 体外酶实验
使用同质时间分辨荧光法测定NVP-TAE684作用于InsR和IGF1R的IC50 值。ATP (10 mM)和20 mg/ml 生物素PolyEY (Glu, Tyr 4:1)，与50 nL NVP-TAE684连续稀释液 (10-500 nM) ，和4 ng InsR 酶，和激酶反应buffer (包括20 mM Tris×HCl, pH 为7.5 /10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA)混合。在室温下温育1小时。加入10 mL检测液终止反应，检测液含50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/ml Eu3+ 穴状化合物标记的磷酸酪氨酸抗体PT66-K,及5 mg/ml 链霉亲和素-XLent。反应进行半小时，在Analyst GT上读取荧光信号。
细胞实验 细胞系 表达Luciferase的Karpas-299, SU-DHL-1,和Ba/F3 细胞，及稳定表达Ba/F3转变的 NPM-ALK, BCR-ABL,或TEL激酶融合构成。
浓度 1 nM-10 μM
孵育时间 2到3天
方法

细胞按每孔2.5×104个接种在384孔板上，和NVP-TAE684的连续稀释液或DMSO温育2到3天。使用Luciferase表达系统测定细胞增殖和存活，然后用Bright-Glo Luciferase 实验系统测评。使用XLFit 软件测定IC50值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP p-ROS1 / ROS1 22240786
Growth inhibition assay Cell viability 18594010
体内研究(In Vivo)
体内研究活性

3和10 mg/kg NVP-TAE684处理4周后,明显减慢淋巴癌生长转移，作用于Karpas-299淋巴癌模型没有毒性。用NVP-TAE684处理Karpas-299 淋巴癌也诱导疾病衰退和下调CD30表达。[1] NVP-TAE684 作用于H3122 CR移植瘤显示出明显的抗癌活性。[2] 用NVP-TAE684处理也提升ALK突变的表现型,尤其是ALKR1275Q。[3]
动物实验 Animal Models 4到6周大的携带Karpas-299移植瘤的雌性Fox Chase SCIDBeige 鼠
Dosages 1, 3, 和 10 mg/kg
Administration 每天口服饲喂，持续3周。
  • https://pubmed.ncbi.nlm.nih.gov/17185414/
  • https://pubmed.ncbi.nlm.nih.gov/21502504/
  • https://pubmed.ncbi.nlm.nih.gov/21838707/

化学信息&溶解度

分子量 614.2 分子式

C30H40ClN7O3S
CAS号 761439-42-3 SDF Download TAE684 (NVP-TAE684) SDF
Smiles CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 10 mg/mL ( (16.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
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 只

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，注：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：取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：取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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