BI-3406 is Potent & Selective SOS1::KRAS Inhibitor (IC50=5 nM), which Opens a New Approach for Treating KRAS-Driven Tumours. BI 3406 selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation. BI 3406 causes RAS GTP and pERK reduction and inhibits cell growth of KRAS mutated cell lines, carrying most of the typical KRAS mutations (i.e. G12D, G12V, G13D and others). BI 3406, when administered orally to tumour bearing mice, causes a dose dependent tumour static effect that can be converted into regressions when combined with MEK1 inhibition
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名称 | BI-3406 |
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Iupac 化学名称 | N-((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)-7-methoxy-2-methyl-6-(((S)-tetrahydrofuran-3-yl)oxy)quinazolin-4-amine |
同义词 | BI-3406; BI 3406; BI3406; |
英文同义词 | BI-3406; BI 3406; BI3406; |
分子式 | C23H25F3N4O3 |
分子量 | 462.4732 |
Smile | C[C@H](C1=CC(N)=CC(C(F)(F)F)=C1)NC2=C3C(C=C(OC)C(O[C@H]4CCOC4)=C3)=NC(C)=N2 |
InChiKey | XVFDNRYZXDHTHT-PXAZEXFGSA-N |
InChi | InChI=1S/C23H25F3N4O3/c1-12(14-6-15(23(24,25)26)8-16(27)7-14)28-22-18-9-21(33-17-4-5-32-11-17)20(31-3)10-19(18)29-13(2)30-22/h6-10,12,17H,4-5,11,27H2,1-3H3,(H,28,29,30)/t12-,17+/m1/s1 |
Cas号 | 2230836-55-0 |
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