Sotorasib (AMG510)

Catalog No.S8830 Batch:S883010

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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 13 mg/mL (23.18 mM)
Water 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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (8.92mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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.

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/

Selleck's Sotorasib (AMG510) Has Been Cited by 64 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
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
Sotorasib resistance triggers epithelial-mesenchymal transition and activates AKT and P38-mediated signaling [ Front Mol Biosci, 2025, 12:1537523] PubMed: 39950162
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
Diet-induced phospholipid remodeling dictates ferroptosis sensitivity and tumorigenesis in the pancreas [ bioRxiv, 2025, 2025.04.04.645324] PubMed: 40235976
Multifactorial stroma-mediated resistance is a major contributor to residual disease under targeted therapies in lung cancers [ Res Sq, 2025, rs.3.rs-6264377] PubMed: 40313737
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

RETURN POLICY
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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.