SOS1-IN-14 是一种有效的、具有选择性和口服活性的SOS1抑制剂，IC50值为 3.9 nM。SOS1-IN-14 可通过 P-糖蛋白介导的外排机制在肠道内被吸收。SOS1-IN-14 可用于研究 KRAS 突变的癌症。SOS1-IN-14 的抑瘤效果优于BI-3406。

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC 50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 [1].

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC 50 of 21 nM [1]. SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC 50 s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction [1].

SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models [1]. SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles [1]. Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs [1]. ICR Mice Sprague–Dawley Rats Beagle Dogs Administration p.o., 50 mg/kg i.v., 2 mg/kg p.o., 10 mg/kg i.v., 2 mg/kg p.o., 20 mg/kg T max (h) 0.5 0.08 3 0.08 2 T 1/2 (h) 4.61 1.17 2.32 3.83 6.68 C max (μg/mL) 2670 1261 265 568 1840 AUC 0-24 (ng/mL·h) 32300 970 1683 2962 25725 CL (mL/min/kg) / 2068 / 11.3 / V ss (L/kg) / 2126 / 3.88 / F (%) / / 34.5 / 86.8 K el (h -1 ) 0.265 / / / / MRT (h) 4.67 / / / / Animal Model: BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models) [1] Dosage: 50 mg/kg Administration: p.o.; q.d., for 21 days Result: Exhibited 83.0% tumor suppression. Showed better potent tumor suppression than BI-3406.

2793405-20-4

C29H29F3N6O2

550.57

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years