产品
编 号：F741711
分子式：C22H24N6O
分子量：388.47
分子式：C22H24N6O
分子量：388.47
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2654743-22-1
产品详情
生物活性：
MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
体内研究：
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 SpeciesParameterRouteDose (mg/kg)Cl (mL/min/kg)Vd,ss (L/kg)T1/2(iv) (h)F (%)
MouseIV/PO3/304.40.281.369
RatIV/PO1/1014.60.280.6283
DogIV/PO2/107.60.480.8638
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.
体外研究：
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 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
体内研究：
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 SpeciesParameterRouteDose (mg/kg)Cl (mL/min/kg)Vd,ss (L/kg)T1/2(iv) (h)F (%)
MouseIV/PO3/304.40.281.369
RatIV/PO1/1014.60.280.6283
DogIV/PO2/107.60.480.8638
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.
体外研究：
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.
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