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SOS1 inhibitor SL43

Chemical Structure : SOS1 inhibitor SL43

CAS No.:

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 449.04
分子式 C27H33ClN4
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

(R)-N4-(1-(4-chlorophenyl)ethyl)-6-(cyclohex-1-en-1-yl)-N2-neopentylquinazoline-2,4-diamine

参考文献

1. Liu X, et al. Bioorg Chem. 2026 Apr 2;175:109823.

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