MRTX-1257 _Ras 抑制劑 - 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作靶點: Ras作通路: GPCR/G Protein儲存式: -20C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實驗 DMSO : 55 mg/mL (97.22 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可

3、以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.68 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.68 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 M

4、RTX-1257選擇性的、不可逆的、共價的并具有服活性的 KRAS G12C 抑制劑，其在 H358 細(xì)胞中測得KRAS 依賴 ERK 磷酸化的 IC50 值為 900 pM。IC50 & Target KRAS(G12C)體內(nèi)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