For research use only.
CAS No. 2296729-00-3
Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
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|Description||Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.|
AMG 510 inhibits SOS1-catalyzed nucleotide exchange of recombinant mutant KRAS (G12C/C118A) but had minimal effect on KRAS (C118A). AMG 510 also selectively impairs the viability of KRAS p.G12C mutant lines but does not affect cell lines with other KRAS mutations.
In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS (G12C), providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Dosed orally (once daily) as a single agent, AMG 510 is capable of inducing tumor regression in mouse models of KRASG12C cancer.
|In vitro||DMSO||100 mg/mL (178.38 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
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Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04887064||Not yet recruiting||Drug: Sotorasib||Hepatic Impairment||Amgen||May 14 2021||Phase 1|
|NCT04380753||Recruiting||Drug: AMG 510||Advanced/Metastatic Solid Tumors With KRAS p.G12C Mutation||Amgen||April 28 2020||Phase 1|
|NCT03600883||Recruiting||Drug: AMG 510|Drug: Anti PD-1/L1|Drug: Midazolam||KRAS p.G12C Mutant Advanced Solid Tumors||Amgen||August 27 2018||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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