MRTX0902

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MRTX0902 是一种有效的高选择性 SOS1 抑制剂，IC50 为 46 nM，Ki 为 2 nM。

MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.(In Vitro):In the MIA PaCa-2 xenograft model of mice, MRTX0902 (25 and 50 mg/kg; p.o.) shows anti-tumor effects and reduces tumor growth by 41% and 53%, respectively.

MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Clint value of 195 mL/min/kg in human liver microsome and a low lipophilicity with cLogP of 3.4.MRTX0902 displays high selectivity on SOS1 (Ki=2 nM) over SOS2 and EGFR (both Ki values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC50 value of 29 nM.

MRTX0902 (compound 32) (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression.MRTX0902 (1-3 mg/kg for i.v. or 10-30 mg/kg for p.o.; single dose) exhibits good brain penetrance, low clearance, and high bioavailability.PK Parameters for MRTX0902 across Species.Animal Model:Female CD-1 mice Dosage:50 mg/kg Administration:Oral gavage; twice daily; 1 day Result:Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5).Showed short half-life of the compound in mice (T1/2?= 1.3 h). Animal Model:MIA PaCa-2 xenograft model in mouse Dosage:25 mg/kg; 50 mg/kg Administration:Oral gavage; twice daily; 25 days Result:Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.

UNII-CRG69FR93G

MAPK/ERK Signaling

Raf

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2654743-22-1

388.47

C22H24N6O

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (32.18 mM)

N([C@H](C)C1=C(C)C(C#N)=CC=C1)C=2C3=C(C=NC(=C3)N4CCOCC4)C(C)=NN2

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(-20℃)

With Ice Pack

≥ 2 years