BI 882370 |CAS:1392429-79-6 Probechem Biochemicals

Chemical Structure : BI 882370

CAS No.: 1392429-79-6

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BI 882370 (BI882370)

货号: PC-63557Not For Human Use, Lab Use Only.

BI 882370 is a highly potent, selective, orally active pan-RAF inhibitor with IC50 of 0.4, 0.8 and 0.6 nM for BRAF V600E, BRAF WT and CRAF, respectively.

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25 mg	￥2680	In stock
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生物&药学活性

BI 882370 is a highly potent, selective, orally active pan-RAF inhibitor with IC50 of 0.4, 0.8 and 0.6 nM for BRAF V600E, BRAF WT and CRAF, respectively.
BI 882370 demonstrates excellent selectivity (>100-fold) against a panel of 253 kinases (The most sensitive kinase CSF1R IC50=39 nM).
BI 882370 binds to the DFG-out (inactive) conformation of the BRAF kinase, unlike vemurafenib and dabrafenib.
BI 882370 reduces p-MEK1/2 and p-ERK1/2 signals in BRAFV600E mutation A375 cells (EC50=0.3 nM), inhibits cell proliferation of a panel BRAF-mutant human melanoma and colorectal cancer cell lines (EC50=1-10 nM).
BI 882370 demonstrates in vivo anti-cancer activity against human melanoma xenografts in nude mice.

物理化学性质&存储条件

分子量	569.676
分子式	C28H33F2N7O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Propane-1-sulfonic acid (3-{5-[(1-ethyl-piperidin-4-yl)-methyl-amino]-3-pyrimidin-5-yl-pyrrolo[3,2-b]pyridin-1-yl}-2,4-difluoro-phenyl)-amide

参考文献

1. Waizenegger IC, et al. Mol Cancer Ther. 2016 Mar;15(3):354-65.

2. Stadtmueller H, et al. New azyindolylphenyl sulfonamides as serine/threonine kinase inhibitors). WO2012/104388 A1. 2012.

BI 882370 (BI882370)

生物&药学活性

物理化学性质&存储条件

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BI 882370 (BI882370)

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物理化学性质&存储条件

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