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Chemical Structure : BI-3406
CAS No.: 2230836-55-0
Catalog No.: PC-38296Not For Human Use, Lab Use Only.
BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
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|---|---|---|---|
| 10 mg | $268 | In stock | |
| 25 mg | $458 | In stock | |
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| 200 mg | Get quote | ||
| 1 g | Get quote |
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BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
BI-3406 selectively disrupted the protein-protein interaction between K-RasG12C or K-RasG12D with SOS1 over SOS2, inhibited RAS-GTP levels with an IC50 of 83–231 nM in SOS1/KRAS-dependent NCI-H358 (KRAS G12C) and A549 (KRAS G12S) cell, reduces pERK levels in RAS-mutated cell lines with IC50 of 17-57 nM.
BI-3406 reduces formation of GTP-loaded RAS and limits cellular proliferation of a broad range of KRAS-driven cancers.
BI-3406 attenuates feedback reactivation induced by MEK inhibitors and enhances sensitivity of KRAS-dependent cancers to MEK inhibition.
Combined SOS1 and MEK inhibition represents a novel and effective therapeutic concept to address KRAS-driven tumors.
| M.Wt | 462.473 | |
| Formula | C23H25F3N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine |
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1. Hofmann MH, et al. Cancer Discov. 2021 Jan;11(1):142-157.
2. HRamharter J, et al. J Med Chem. 2021 May 27;64(10):6569-6580.
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