AMG-510 - KRAS G12C 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAMG-510Cat. No.: HY-114277分式: CHFNO分量: 560.59作靶點: Ras作通路: GPCR/G Protein儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據體外實驗 DMSO : 125 mg/mL (222.98 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration

2、制備儲備液1 mM 1.7838 mL 8.9192 mL 17.8383 mL5 mM 0.3568 mL 1.7838 mL 3.5677 mL10 mM 0.1784 mL 0.8919 mL 1.7838 mL請根據產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。體內實驗 請根據您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據儲存條件，適當保存；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% D

3、MSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.71 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.71 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.71 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Sm

4、all Molecules 您邊的抑制劑師www.MedChemE物活性 AMG-510種有效的，服物可利的，選擇性的 KRAS G12C 共價抑制劑，將 KRAS G12C 鎖定在活躍的 GDP 約束狀態(tài)。AMG-510 選擇性靶向的 KRAS p.G12C 突變體，具有抗腫瘤活性 1 2。IC50 & Target KRAS(G12C)體外研究 In cellular assays, AMG 510 covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measuredby phosphorylation of

5、ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines 2.體內研究 In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS G12C, providing durablesuppression of the mitogen-activated protein kinase (MAPK) signaling pathway. AMG 510 (orally; once daily)is capable of inducing tumor regress

6、ion in mouse models of KRAS G12C cancer 3.REFERENCES1. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel smallmolecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.2. Karen Rex, et al. Abstract

7、 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small moleculeinhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.3. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solidtumors. Cancer Chemistry.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc