PF-4708671
PF-4708671是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。
PF-4708671 Chemical Structure
CAS: 1255517-76-0
产品质控
批次：
纯度：
99.91%
99.91
PF-4708671相关产品
| 相关靶点 | p70 S6K p70 S6K1 RSK1 RSK2 RSK3 RSK4 | 点击展开 |
|---|---|---|
| 相关产品 | BI-D1870 LY2584702 LY2584702 Tosylate LJI308 LJH685 Phospho-S6K1(T421/S424) Rabbit Recombinant mAb | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 点击展开 |
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 |
|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | SANGER | ||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | SANGER | ||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | SANGER | ||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | SANGER | ||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | SANGER | ||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | SANGER | ||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | SANGER | ||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | SANGER | ||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PF-4708671是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | PF-4708671是一种哌嗪基嘧啶类似物，是第一个S6K1特异性抑制剂。PF-4708671不显著抑制紧密相关的S6K2亚型或一组其他AGC激酶 (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 或SGK1)的活性。PF-4708671抑制S6K1介导的响应IGF-1（胰岛素样生长因子1）的S6蛋白的磷酸化，对PMA-诱导的底物磷酸化没有作用效果，底物与RSK (p90核糖体S6激酶)和MSK（丝分裂原和应激活化蛋白激酶）激酶高度相关。PF-4708671诱导S6K1的T型环和疏水性基序磷酸化，这种作用依赖于mTORC1 (mTOR复合体1)。PF-4708671不影响mTORC1的活性。[1] | |||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K |
|
28626016 | |
| Growth inhibition assay | Cell viability |
|
30423811 | |
化学信息&溶解度
| 分子量 | 390.41 | 分子式 | C19H21F3N6 |
| CAS号 | 1255517-76-0 | SDF | Download PF-4708671 SDF |
| Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
Ethanol : 40 mg/mL (102.45 mM) DMSO : 30 mg/mL ( (76.84 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 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
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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常见问题及建议解决方法
问题 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?
回答：
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.
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