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Chemical Structure : BI 882370
CAS No.: 1392429-79-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $268 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 569.676 | |
| Formula | C28H33F2N7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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