Home Cell Cycle Ras inhibitor Sotorasib (AMG510) For research use only.

Sotorasib (AMG510)

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

Sotorasib (AMG510) Chemical Structure

Sotorasib (AMG510) Chemical Structure

CAS: 2296729-00-3

Selleck's Sotorasib (AMG510) has been cited by 34 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Sotorasib (AMG510)

Adagrasib (MRTX849)

Sotorasib and Adagrasib increase CD3/4/8+ T-cell tumor infiltration and decrease myeloid suppressor cell populations in vivo.

Rosen JC, et al. Ther Adv Med Oncol. 2023 Mar 16;15:17588359231160141.

ARS-1620

Sotorasib and ARS-1620 are KRAS inhibitors that offer the potential to overcome resistance mechanisms in KRAS-driven cancers.

Wang Z, et al. Mol Biomed. 2022 Dec 12;3(1):42.

Osimertinib (AZD9291)

Sotorasib and Osimertinib encounter resistance to doxycycline-induced MET overexpression in NCI-H358/HCC827 cells.

Reischmann N, et al. iScience. 2023 May 29;26(7):107006.

Trametinib (GSK1120212)

Sotorasib and Trametinib combination suppress tumor growth in mice bearing patient-derived xenografts.

Zhao Y, et al. Nature. 2021;599(7886):679-683.

Tepotinib

Tepotinib and Sotorasib combination significantly inhibits tumor growth and results in tumor regression in mice bearing subcutaneous NCI-H358 tetON-MET xenografts.

Reischmann N, et al. iScience. 2023 May 29;26(7):107006.

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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
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].
Cell Research Cell lines HBEC30KT cells
Concentrations 1 uM
Incubation Time 48 h
Method

Cells were treated with AMG-510 (1 μM) or DMSO for 48 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ERK EGFR / AKT / MEK / ERK / Vinculin EGFR / RAS / MEK / DUSP6 / CyclinD1 / Vinculin pMEK / pERK / pAKT / HSP90 32430388
In Vivo
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].
Animal Research Animal Models Female ICR-SCID mice
Dosages 100 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06061523 Not yet recruiting Healthy Participants Amgen April 15 2024 Phase 1
NCT05920356 Recruiting Non-Small Cell Lung Cancer (NSCLC) Amgen November 16 2023 Phase 3
NCT05497557 Completed Healthy Volunteers Amgen August 4 2022 Phase 1
NCT05400577 Withdrawn Non-Small Cell Lung Cancer Fox Chase Cancer Center July 13 2022 Phase 2
NCT05480865 Recruiting Solid Tumor Adult|Metastatic Solid Tumor|Metastatic NSCLC|Non Small Cell Lung Cancer Navire Pharma Inc. a BridgeBio company|Amgen July 6 2022 Phase 1

Chemical lnformation & Solubility

Molecular Weight 560.59 Formula

C30H30F2N6O3
CAS No. 2296729-00-3 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (178.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

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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