MRTX-1257 _Ras 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMRTX-1257Cat. No.: HY-114436CAS No.: 2206736-04-9分式: CHNO分量: 565.71作靶点: Ras作通路: GPCR/G Protein储存式: -20C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性数据体外实验 DMSO : 55 mg/mL (97.22 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7677 mL 8.8385 mL 17.6769 mL5 mM 0.3535 mL 1.7677 mL 3.5354 mL10 mM 0.1768 mL 0.8838 mL 1.7677 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可

3、以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.68 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.68 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 M

4、RTX-1257选择性的、不可逆的、共价的并具有服活性的 KRAS G12C 抑制剂，其在 H358 细胞中测得KRAS 依赖 ERK 磷酸化的 IC50 值为 900 pM。IC50 & Target KRAS(G12C)体内研究 MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapidtumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in m

5、ice 1.MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups 1.MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained 70 days aftercessation of treatment 1.Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse) 1.Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30

6、mg/kg and 100 mg/kg.Administration: Orally daily for 30 days.Result: Showed rapid tumor growth inhibition at all dose groups.Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.100 mg/kg daily led to complete responses that are maintained 70 days after cessation oftreatment.REFERENCES1. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in AnimalModels of Cancer.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only