AMG 510 (Sotorasib)

Catalog No.S8830 Batch:S883007

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Technical Data

Formula

C30H30F2N6O3
Molecular Weight 560.59 CAS No. 2296729-00-3
Solubility (25°C)* In vitro DMSO 50 mg/mL (89.19 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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)
In vitro

Sotorasib (AMG510) inhibits SOS1-catalyzed nucleotide exchange of recombinant mutant KRAS (G12C/C118A) but had minimal effect on KRAS (C118A). It also selectively impairs the viability of KRAS p.G12C mutant lines but does not affect cell lines with other KRAS mutations.
In Vivo

In preclinical tumour models, Sotorasib (AMG510) rapidly and irreversibly binds to KRAS (G12C), providing durable suppression of the mitogen-activated protein kinase (MAPK) signalling pathway. Dosed orally (once daily) as a single agent, it is capable of inducing tumour regression in mouse models of KRASG12C cancer.

Protocol (from reference)

Cell Assay:

[3]
  • Cell Lines

    HBEC30KT cells

  • Concentrations

    1 uM

  • Incubation Time

    48 h

  • Method

    Cells were treated with Sotorasib (AMG510) (1 μM) or DMSO for 48 h.
Animal Study:

[4]
  • Animal Models

    Female ICR-SCID mice

  • Dosages

    100 mg/kg

  • Administration

    o.g.

References

  • http://cancerres.aacrjournals.org/content/79/13_Supplement/4484.short
  • http://cancerres.aacrjournals.org/content/79/13_Supplement/4455.short
  • https://pubmed.ncbi.nlm.nih.gov/35838183/
  • https://pubmed.ncbi.nlm.nih.gov/35573474/

Sellecks AMG 510 (Sotorasib) Has Been Cited by 65 Publications

Oncogenic RAS induces a distinctive form of non-canonical autophagy mediated by the P38-ULK1-PI4KB axis [ Cell Res, 2025, 10.1038/s41422-025-01085-9] PubMed: 40055523
Targeting CDK12/13 Drives Mitotic Arrest to Overcome Resistance to KRASG12C Inhibitors [ Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0450] PubMed: 41165466
WEE1 inhibitor exerts synergistic effect with KRAS G12C inhibitor via MYBL2-RRM2 axis in KRASG12C-mutant lung cancer [ Cell Death Dis, 2025, 16(1):661] PubMed: 40885709
Modeling response to the KRAS-G12C inhibitor AZD4625 in KRASG12C NSCLC patient-derived xenografts reveals insights into primary resistance mechanisms [ Br J Cancer, 2025, 10.1038/s41416-025-03216-w] PubMed: 41076489
Sotorasib resistance triggers epithelial-mesenchymal transition and activates AKT and P38-mediated signaling [ Front Mol Biosci, 2025, 12:1537523] PubMed: 39950162
Quantifying small GTPase activation status using a novel fluorescence HPLC-based assay [ J Biol Chem, 2025, 301(6):108545] PubMed: 40286847
Biophysical and structural analysis of KRAS switch-II pocket inhibitors reveals allele-specific binding constraints [ J Biol Chem, 2025, 301(7):110331] PubMed: 40473215
Detection of PIP2 distributions in biological membranes using a peptide-based sensor [ J Biol Chem, 2025, S0021-9258(25)02678-X] PubMed: 41109350
LC-MS/MS method development and validation for novel targeted anticancer therapies adagrasib, capmatinib, ensartinib, entrectinib, larotrectinib, lorlatinib, pralsetinib, selpercatinib and sotorasib [ J Pharm Biomed Anal, 2025, 266:117078] PubMed: 40743983
Diet-induced phospholipid remodeling dictates ferroptosis sensitivity and tumorigenesis in the pancreas [ bioRxiv, 2025, 2025.04.04.645324] PubMed: 40235976

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.