Sotorasib (AMG510)

Catalog No.S8830

For research use only.

Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.

Sotorasib (AMG510) Chemical Structure

CAS No. 2296729-00-3

Selleck's Sotorasib (AMG510) has been cited by 9 Publications

Purity & Quality Control

Choose Selective Ras Inhibitors

Biological Activity

Description Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
Targets
K-Ras(G12C) [1]
()
In vitro

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[1].

Assay
Methods Test Index PMID
Western blot ERK ; EGFR / AKT / MEK / ERK / Vinculin ; EGFR / RAS / MEK / DUSP6 / CyclinD1 / Vinculin ; pMEK / pERK / pAKT / HSP90 32430388 33655066
In vivo

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[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(178.38 mM)
Water Insoluble
Ethanol '100 mg/mL

Chemical Information

Molecular Weight 560.59
Formula

C30H30F2N6O3

CAS No. 2296729-00-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CN(CCN1C2=NC(=O)N(C3=NC(=C(C=C32)F)C4=C(C=CC=C4F)O)C5=C(C=CN=C5C(C)C)C)C(=O)C=C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04933695 Not yet recruiting Drug: Sotorasib Non-small Cell Lung Cancer Amgen January 24 2022 Phase 2
NCT05074810 Not yet recruiting Drug: VS-6766 and sotorasib Non Small Cell Lung Cancer|KRAS Activating Mutation Verastem Inc.|Amgen December 2021 Phase 1|Phase 2
NCT05054725 Recruiting Drug: RMC-4630|Drug: Sotorasib Non-Small Cell Lung Cancer Revolution Medicines Inc.|Sanofi|Amgen December 2021 Phase 2
NCT05048784 Recruiting Drug: Sotorasib Healthy Participants Amgen September 13 2021 Phase 1
NCT05045638 Completed Drug: Rosuvastatin|Drug: Sotorasib Healthy Participants Amgen September 9 2021 Phase 1
NCT04887064 Recruiting Drug: Sotorasib Hepatic Impairment Amgen May 12 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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