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 。$
| Cas No. | 2793405-20-4 |
| 分子式 | C29H29F3N6O2 |
| 分子量 | 550.57 |
| 溶解度 | DMSO : 250 mg/mL (454.07 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SOS1-IN-14 is a potent, selective and orally activeSOS1inhibitor with anIC50value 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 thanBI-3406[1]. SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50of 21 nM[1].
SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s 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 | | Tmax(h) | 0.5 | 0.08 | 3 | 0.08 | 2 | | T1/2(h) | 4.61 | 1.17 | 2.32 | 3.83 | 6.68 | | Cmax(μg/mL) | 2670 | 1261 | 265 | 568 | 1840 | | AUC0-24(ng/mL.h) | 32300 | 970 | 1683 | 2962 | 25725 | | CL (mL/min/kg) | / | 2068 | / | 11.3 | / | | Vss(L/kg) | / | 2126 | / | 3.88 | / | | F (%) | / | / | 34.5 | / | 86.8 | | Kel(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 thanBI-3406. |
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