Sotorasib

2296729-00-3

560.59

H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH); DMSO : 50 mg/mL (89.19 mM; Need ultrasonic)

GPCR/G Protein

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors^[1][2]. IC50 & Target: KRAS G12C^[1] In Vitro: In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines^[2].
Sotorasib (AMG-510; 1-10 uM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC₅₀?0.006 uM and 0.009 uM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC₅₀>7.5 uM)^[3]. In Vivo: In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer^[3].