• 產(chǎn)品描述： MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10)

• 靶點(diǎn)： KRAS-SOS1:46 nM (IC50);Raf

• 體外研究：
  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.

• 體內(nèi)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. 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.

• 參考文獻(xiàn)：
  1. Ketcham JM, et al. Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 2022 Jul 28;65(14):9678-9690.

• 溶解性： soluble  in  DMSO

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.574 ml	12.871 ml	25.742 ml
  5 mM	0.515 ml	2.574 ml	5.148 ml
  10 mM	0.257 ml	1.287 ml	2.574 ml
  50 mM	0.051 ml	0.257 ml	0.515 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *