Chemical Structure : SOS1 inhibitor SL43
货号: PC-26521Not For Human Use, Lab Use Only.
SOS1 inhibitor SL43 is a potent, selective and orally bioavailable SOS1 inhibitor with binding KD of 0.16 uM, potently disrupts the SOS1-KRASG12C interaction with IC50 of 13 nM, broadly inhibits SOS1-mediated nucleotide exchange on multiple KRAS mutants (G12C, G12V and G12D; IC50 = 13.4-29.1 nM).
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SOS1 inhibitor SL43 is a potent, selective and orally bioavailable SOS1 inhibitor with binding KD of 0.16 uM, potently disrupts the SOS1-KRASG12C interaction with IC50 of 13 nM, broadly inhibits SOS1-mediated nucleotide exchange on multiple KRAS mutants (G12C, G12V and G12D; IC50 = 13.4-29.1 nM).
SL43 exhibited potent and selective antiproliferative activity against KRAS-mutant colorectal cancer cells (IC50 = 0.028–0.238 μM), achieving over 100-fold selectivity over KRAS wild-type cells.
SL43 (20 and 40 mg/kg, p.o.) also significantly suppressed tumor growth (TGI = 57.2% and 74.9%, respectively), outperforming MRTX0902 (60 mg/kg, TGI = 47.1%) with no observable systemic toxicity.
| 分子量 | 449.04 | |
| 分子式 | C27H33ClN4 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Liu X, et al. Bioorg Chem. 2026 Apr 2;175:109823.
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