Sotorasib (AMG510)

Catalog No.S8830 Batch:S883006

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Technical Data

Formula

C30H30F2N6O3
Molecular Weight 560.59 CAS No. 2296729-00-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (178.38 mM)
Ethanol 15 mg/mL (26.75 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].
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)

Cell Assay:

[3]
  • 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.
Animal Study:

[4]
  • Animal Models

    Female ICR-SCID mice

  • Dosages

    100 mg/kg

  • Administration

    o.g.

Selleck's Sotorasib (AMG510) has been cited by 45 publications

Base editing screens define the genetic landscape of cancer drug resistance mechanisms [ Nat Genet, 2024, 10.1038/s41588-024-01948-8] PubMed: 39424923
Engineered a dual-targeting HA-TPP/A nanoparticle for combination therapy against KRAS-TP53 co-mutation in gastrointestinal cancers [ Bioact Mater, 2024, 32:277-291] PubMed: 37876556
Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer [ Nat Commun, 2024, 15(1):6076] PubMed: 39025835
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] PubMed: 38508142
Molecular basis for antibody recognition of multiple drug-peptide/MHC complexes [ Proc Natl Acad Sci U S A, 2024, 121(22):e2319029121] PubMed: 38781214
AXL signal mediates adaptive resistance to KRAS G12C inhibitors in KRAS G12C-mutant tumor cells [ Cancer Lett, 2024, 587:216692] PubMed: 38342232
Hedgehog signalling is involved in acquired resistance to KRASG12C inhibitors in lung cancer cells [ Cell Death Dis, 2024, 15(1):56] PubMed: 38225225
KRASG 12C-inhibitor-based combination therapies for pancreatic cancer: insights from drug screening [ Mol Oncol, 2024, 10.1002/1878-0261.13725] PubMed: 39253995
RECK/GPR124-driven WNT signaling in pancreatic and gastric cancer cells [ Cancer Sci, 2024, 10.1111/cas.16258] PubMed: 38923741
A drug discovery pipeline for MAPK/ERK pathway inhibitors in C. elegans [ Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221] PubMed: 39212544

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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