|N-(3-((5-碘-4-((3-(噻吩-2-甲酰胺基)丙基)氨基)嘧啶-2-基)氨基)苯基)吡咯烷-1-甲酰胺|CsnPharm

CAS No.: 702675-74-9

BX795 Catalog No. CSN12711

Synonyms: BX795游离态

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively, also inhibit Aurora B and IκB kinase ε (IKKε).

规格	价格	促销价格	库存	数量

400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 c-Kit

IC50:320nM GSK-3β

IC50:620nM PDK-1

IC50:6nM PKA

IC50:840nM
描述The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs^[3]. BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor with an IC₅₀ value of 26 nM. BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis^[3]. When treating asynchronously growing cultures of tumor cells for 18 h with 10 μM BX-912, it promoted a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G₂/M phase of the cell cycle. BX-912 also potently inhibited the growth of HCT-116 and PC-3 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM for HCT-116 and IC₅₀ value of 0.32 μM for PC-3^[3].
作用机制BX-795 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that it binds to the ATP binding pocket of PDK1^[2].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human 5637 cell	-	Growth inhibition assay	-	Inhibition of human 5637 cell growth in a cell viability assay, IC50=8.07904 μM	SANGER
human 697 cell	-	Growth inhibition assay	-	Inhibition of human 697 cell growth in a cell viability assay, IC50=1.01623 μM	SANGER
human 8-MG-BA cell	-	Growth inhibition assay	-	Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=1.95744 μM	SANGER

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6907 mL
- 8.4535 mL
- 16.9071 mL
- 5 mM
- 0.3381 mL
- 1.6907 mL
- 3.3814 mL
- 10 mM
- 0.1691 mL
- 0.8454 mL
- 1.6907 mL

技术信息

CAS号

702675-74-9

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H26IN7O2S

运输

蓝冰

分子量

591.47

别名

BX795游离态

溶解度

DMSO	26.0 mg/mL (44.0 mM) warming
Water	insoluble

动物实验配方

2% DMSO+30% PEG +2% Tween 80+water

4 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human 5637 cell	-	Growth inhibition assay	-	Inhibition of human 5637 cell growth in a cell viability assay, IC50=8.07904 μM	SANGER
human 697 cell	-	Growth inhibition assay	-	Inhibition of human 697 cell growth in a cell viability assay, IC50=1.01623 μM	SANGER
human 8-MG-BA cell	-	Growth inhibition assay	-	Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=1.95744 μM	SANGER
human A172 cell	-	Growth inhibition assay	-	Inhibition of human A172 cell growth in a cell viability assay, IC50=4.4457 μM	SANGER
human A204 cell	-	Growth inhibition assay	-	Inhibition of human A204 cell growth in a cell viability assay, IC50=1.15467 μM	SANGER
human A2058 cell	-	Growth inhibition assay	-	Inhibition of human A2058 cell growth in a cell viability assay, IC50=2.97844 μM	SANGER
human A253 cell	-	Growth inhibition assay	-	Inhibition of human A253 cell growth in a cell viability assay, IC50=4.18893 μM	SANGER
human A375 cell	-	Growth inhibition assay	-	Inhibition of human A375 cell growth in a cell viability assay, IC50=1.30858 μM	SANGER
human A388 cell	-	Growth inhibition assay	-	Inhibition of human A388 cell growth in a cell viability assay, IC50=21.1398 μM	SANGER
human A3-KAW cell	-	Growth inhibition assay	-	Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=0.73055 μM	SANGER
human A427 cell	-	Growth inhibition assay	-	Inhibition of human A427 cell growth in a cell viability assay, IC50=1.73589 μM	SANGER
human A498 cell	-	Growth inhibition assay	-	Inhibition of human A498 cell growth in a cell viability assay, IC50=4.56383 μM	SANGER
human A549 cell	-	Growth inhibition assay	-	Inhibition of human A549 cell growth in a cell viability assay, IC50=2.13808 μM	SANGER
human AGS cell	-	Growth inhibition assay	-	Inhibition of human AGS cell growth in a cell viability assay, IC50=2.56257 μM	SANGER
human ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.06073 μM	SANGER
human AN3-CA cell	-	Growth inhibition assay	-	Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.63991 μM	SANGER
human ATN-1 cell	-	Growth inhibition assay	-	Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=1.37185 μM	SANGER
human BCPAP cell	-	Growth inhibition assay	-	Inhibition of human BCPAP cell growth in a cell viability assay, IC50=2.23158 μM	SANGER
human BE-13 cell	-	Growth inhibition assay	-	Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.70477 μM	SANGER
human Becker cell	-	Growth inhibition assay	-	Inhibition of human Becker cell growth in a cell viability assay, IC50=3.01112 μM	SANGER
human BFTC-905 cell	-	Growth inhibition assay	-	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=1.08101 μM	SANGER
human BHT-101 cell	-	Growth inhibition assay	-	Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=1.57877 μM	SANGER
human C32 cell	-	Growth inhibition assay	-	Inhibition of human C32 cell growth in a cell viability assay, IC50=1.7639 μM	SANGER
human Ca9-22 cell	-	Growth inhibition assay	-	Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50=2.12847 μM	SANGER
human CAKI-1 cell	-	Growth inhibition assay	-	Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=2.28058 μM	SANGER
human CAL-51 cell	-	Growth inhibition assay	-	Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=1.22156 μM	SANGER
human CAS-1 cell	-	Growth inhibition assay	-	Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=3.01569 μM	SANGER
human CHL-1 cell	-	Growth inhibition assay	-	Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=1.92379 μM	SANGER
human CHP-134 cell	-	Growth inhibition assay	-	Inhibition of human CHP-134 cell growth in a cell viability assay, IC50=1.94467 μM	SANGER
human CHP-212 cell	-	Growth inhibition assay	-	Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=1.14037 μM	SANGER
human COLO-800 cell	-	Growth inhibition assay	-	Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=2.05136 μM	SANGER
human CTB-1 cell	-	Growth inhibition assay	-	Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=2.39761 μM	SANGER
human D-263MG cell	-	Growth inhibition assay	-	Inhibition of human D-263MG cell growth in a cell viability assay, IC50=2.38327 μM	SANGER
human D-283MED cell	-	Growth inhibition assay	-	Inhibition of human D-283MED cell growth in a cell viability assay, IC50=1.03948 Μm	SANGER
human D-423MG cell	-	Growth inhibition assay	-	Inhibition of human D-423MG cell growth in a cell viability assay, IC50=1.60806 μM	SANGER
human D-566MG cell	-	Growth inhibition assay	-	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=1.30448 μM	SANGER
human DB cell	-	Growth inhibition assay	-	Inhibition of human DB cell growth in a cell viability assay, IC50=2.12631 μM	SANGER
human DK-MG cell	-	Growth inhibition assay	-	Inhibition of human DK-MG cell growth in a cell viability assay, IC50=1.57298 μM	SANGER
human DOHH-2 cell	-	Growth inhibition assay	-	Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.45814 μM	SANGER
human DU-4475 cell	-	Growth inhibition assay	-	Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=1.29245 μM	SANGER
human EM-2 cell	-	Growth inhibition assay	-	Inhibition of human EM-2 cell growth in a cell viability assay, IC50=2.35337 μM	SANGER
human ES1 cell	-	Growth inhibition assay	-	Inhibition of human ES1 cell growth in a cell viability assay, IC50=1.75451 μM	SANGER
human ES3 cell	-	Growth inhibition assay	-	Inhibition of human ES3 cell growth in a cell viability assay, IC50=2.62285 μM	SANGER
human ES5 cell	-	Growth inhibition assay	-	Inhibition of human ES5 cell growth in a cell viability assay, IC50=1.19354 μM	SANGER
human ES7 cell	-	Growth inhibition assay	-	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.83566 μM	SANGER
human ES8 cell	-	Growth inhibition assay	-	Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.84336 μM	SANGER
human G-401 cell	-	Growth inhibition assay	-	Inhibition of human G-401 cell growth in a cell viability assay, IC50=2.56099 μM	SANGER
human G-402 cell	-	Growth inhibition assay	-	Inhibition of human G-402 cell growth in a cell viability assay, IC50=1.46525 μM	SANGER
human GI-ME-N cell	-	Growth inhibition assay	-	Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=1.8653 μM	SANGER
human GT3TKB cell	-	Growth inhibition assay	-	Inhibition of human GT3TKB cell growth in a cell viability assay, IC50=1.89642 μM	SANGER
human H4 cell	-	Growth inhibition assay	-	Inhibition of human H4 cell growth in a cell viability assay, IC50=1.10201 μM	SANGER
human HCC1187 cell	-	Growth inhibition assay	-	Inhibition of human HCC1187 cell growth in a cell viability assay, IC50=2.89677 μM	SANGER
human HL-60 cell	-	Growth inhibition assay	-	Inhibition of human HL-60 cell growth in a cell viability assay, IC50=2.54159 μM	SANGER
human HN cell	-	Growth inhibition assay	-	Inhibition of human HN cell growth in a cell viability assay, IC50=2.12198 μM	SANGER
human HO-1-N-1 cell	-	Growth inhibition assay	-	Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50=1.97117 μM	SANGER
human HOP-92 cell	-	Growth inhibition assay	-	Inhibition of human HOP-92 cell growth in a cell viability assay, IC50=1.27293 μM	SANGER
human HOS cell	-	Growth inhibition assay	-	Inhibition of human HOS cell growth in a cell viability assay, IC50=1.57309 μM	SANGER
human Hs-578-T cell	-	Growth inhibition assay	-	Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=2.41587 μM	SANGER
human HSC-3 cell	-	Growth inhibition assay	-	Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=1.44208 μM	SANGER
human HuO-3N1 cell	-	Growth inhibition assay	-	Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=2.60307 μM	SANGER
human HuO9 cell	-	Growth inhibition assay	-	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=2.56456 μM	SANGER
human IST-SL1 cell	-	Growth inhibition assay	-	Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=2.32174 μM	SANGER
human JVM-3 cell	-	Growth inhibition assay	-	Inhibition of human JVM-3 cell growth in a cell viability assay, IC50=1.86491 μM	SANGER
human KG-1 cell	-	Growth inhibition assay	-	Inhibition of human KG-1 cell growth in a cell viability assay, IC50=2.27792 μM	SANGER
human KGN cell	-	Growth inhibition assay	-	Inhibition of human KGN cell growth in a cell viability assay, IC50=2.22595 μM	SANGER
human KM12 cell	-	Growth inhibition assay	-	Inhibition of human KM12 cell growth in a cell viability assay, IC50=3.30132 μM	SANGER
human KS-1 cell	-	Growth inhibition assay	-	Inhibition of human KS-1 cell growth in a cell viability assay, IC50=1.8298 μM	SANGER
human KYSE-150 cell	-	Growth inhibition assay	-	Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50=2.7297 μM	SANGER
human L-363 cell	-	Growth inhibition assay	-	Inhibition of human L-363 cell growth in a cell viability assay, IC50=1.18197 μM	SANGER
human LAMA-84 cell	-	Growth inhibition assay	-	Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=1.76872 μM	SANGER
human LB1047-RCC cell	-	Growth inhibition assay	-	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=1.29281 μM	SANGER
human LB2241-RCC cell	-	Growth inhibition assay	-	Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=2.69079 μM	SANGER
human LC-2-ad cell	-	Growth inhibition assay	-	Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=1.47132 μM	SANGER
human LOXIMVI cell	-	Growth inhibition assay	-	Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=1.50552 μM	SANGER
human LXF-289 cell	-	Growth inhibition assay	-	Inhibition of human LXF-289 cell growth in a cell viability assay. IC50=0.65693 μM	SANGER
human M059J cell	-	Growth inhibition assay	-	Inhibition of human M059J cell growth in a cell viability assay, IC50=1.37652 μM	SANGER
human MC-IXC cell	-	Growth inhibition assay	-	Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.8953 μM	SANGER
human MDA-MB-157 cell	-	Growth inhibition assay	-	Inhibition of human MDA-MB-157 cell growth in a cell viability assay, IC50=1.71674 μM	SANGER
human MFE-280 cell	-	Growth inhibition assay	-	Inhibition of human MFE-280 cell growth in a cell viability assay, IC50=2.56686 μM	SANGER
human MG-63 cell	-	Growth inhibition assay	-	Inhibition of human MG-63 cell growth in a cell viability assay, IC50=1.68567 μM	SANGER
human MHH-ES-1 cell	-	Growth inhibition assay	-	Inhibition of human MHH-ES-1 cell growth in a cell viability assay, IC50=2.72633 μM	SANGER
human MOLT-4 cell	-	Growth inhibition assay	-	Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=1.03244 μM	SANGER
human MV-4-11 cell	-	Growth inhibition assay	-	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=36.8 nM	SANGER
human NB10 cell	-	Growth inhibition assay	-	Inhibition of human NB10 cell growth in a cell viability assay, IC50=4.22773 μM	SANGER
human NB14 cell	-	Growth inhibition assay	-	Inhibition of human NB14 cell growth in a cell viability assay, IC50=1.06081 μM	SANGER
human NB5 cell	-	Growth inhibition assay	-	Inhibition of human NB5 cell growth in a cell viability assay, IC50=2.93715 μM	SANGER
human NB69 cell	-	Growth inhibition assay	-	Inhibition of human NB69 cell growth in a cell viability assay, IC50=1.15865 μM	SANGER
human NBsusSR cell	-	Growth inhibition assay	-	Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=1.24578 μM	SANGER
human NCI-H1048 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.78509 μM	SANGER
human NCI-H1155 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50=2.69405 μM	SANGER
human NCI-H1755 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=2.54043 μM	SANGER
human NCI-H292 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=2.57722 μM	SANGER
human NCI-H460 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=2.43955 μM	SANGER
human NKM-1 cell	-	Growth inhibition assay	-	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=0.36194 μM	SANGER
human NTERA-S-cl-D1 cell	-	Growth inhibition assay	-	Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=1.07775 μM	SANGER
human OVCAR-5 cell	-	Growth inhibition assay	-	Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50=2.27734 μM	SANGER
human P12-ICHIKAWA cell	-	Growth inhibition assay	-	Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=1.18171 μM	SANGER
human P30-OHK cell	-	Growth inhibition assay	-	Inhibition of human P30-OHK cell growth in a cell viability, IC50=0.4965 μM	SANGER
human PA-1 cell	-	Growth inhibition assay	-	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=0.80422 μM	SANGER
human PC-3 cell	-	Growth inhibition assay	-	Inhibition of human PC-3 cell growth in a cell viability assay, IC50=4.17411 μM	SANGER
human QIMR-WIL cell	-	Growth inhibition assay	-	Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=2.28744 μM	SANGER
human Ramos-2G6-4C10 cell	-	Growth inhibition assay	-	Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=2.23759 μM	SANGER
human RH-1 cell	-	Growth inhibition assay	-	Inhibition of human RH-1 cell growth in a cell viability assay, IC50=1.70274 μM	SANGER
human RS4-11 cell	-	Growth inhibition assay	-	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.72594 μM	SANGER
human SF126 cell	-	Growth inhibition assay	-	Inhibition of human SF126 cell growth in a cell viability assay, IC50=2.43621 μM	SANGER
human SK-NEP-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=1.65376 μM	SANGER
human SK-UT-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=2.29339 μM	SANGER
human SW1088 cell	-	Growth inhibition assay	-	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=1.99673 μM	SANGER
human SW1573 cell	-	Growth inhibition assay	-	Inhibition of human SW1573 cell growth in a cell viability assay, IC50=6.90491 μM	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.29142 μM	SANGER
human SW48 cell	-	Growth inhibition assay	-	Inhibition of human SW48 cell growth in a cell viability assay, IC50=2.02067 μM	SANGER
human SW780 cell	-	Growth inhibition assay	-	Inhibition of human SW780 cell growth in a cell viability assay, IC50=3.25609 μM	SANGER
human SW872 cell	-	Growth inhibition assay	-	Inhibition of human SW872 cell growth in a cell viability assay, IC50=2.70676 μM	SANGER
human SW962 cell	-	Growth inhibition assay	-	Inhibition of human SW962 cell growth in a cell viability assay, IC50=2.33757 μM	SANGER
human SW982 cell	-	Growth inhibition assay	-	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.95124 μM	SANGER
human T98G cell	-	Growth inhibition assay	-	Inhibition of human T98G cell growth in a cell viability assay, IC50=2.38857 μM	SANGER
human TE-11 cell	-	Growth inhibition assay	-	Inhibition of human TE-11 cell growth in a cell viability assay, IC50=1.6528 μM	SANGER
human TI-73 cell	-	Growth inhibition assay	-	Inhibition of human TI-73 cell growth in a cell viability assay, IC50=2.11399 μM	SANGER
human U251 cell	-	Growth inhibition assay	-	Inhibition of human U251 cell growth in a cell viability assay, IC50=28.1175 μM	SANGER
human U-2-OS cell	-	Growth inhibition assay	-	Inhibition of human U-2-OS cell growth in a cell viability assay, IC50=1.58806 μM	SANGER
human UMC-11 cell	-	Growth inhibition assay	-	Inhibition of human UMC-11 cell growth in a cell viability assay, IC50=2.90477 μM	SANGER
human VA-ES-BJ cell	-	Growth inhibition assay	-	Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=0.98467 μM	SANGER
human VM-CUB-1 cell	-	Growth inhibition assay	-	Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50=2.04119 μM	SANGER
human YH-13 cell	-	Growth inhibition assay	-	Inhibition of human YH-13 cell growth in a cell viability assay, IC50=0.62888 μM	SANGER
human YKG-1 cell	-	Growth inhibition assay	-	Inhibition of human YKG-1 cell growth in a cell viability assay, IC50=1.77124 μM	SANGER
KRX cells	-	Function assay	7 mins	Inhibition of SUMO-tagged ULK1 (unknown origin) kinase domain expressed in KRX cells using [32P]-gamma-ATP and myelin basic protein substrate incubated for 7 mins	26275681

靶点	Description	IC50
c-Kit		IC50:320nM
GSK-3β		IC50:620nM
PDK-1		IC50:6nM
PKA		IC50:840nM

BX795 Catalog No. CSN12711

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