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)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml 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.

Selleck's Sotorasib (AMG510) has been cited by 37 publications

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
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] PubMed: 38508142
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
Molecular Characterization of Acquired Resistance to KRASG12C-EGFR Inhibition in Colorectal Cancer [ Cancer Discov, 2023, 13(1):41-55] PubMed: 36355783
LKB1-Dependent Regulation of TPI1 Creates a Divergent Metabolic Liability between Human and Mouse Lung Adenocarcinoma [ Cancer Discov, 2023, 13(4):1002-1025] PubMed: 36715544
LKB1-Dependent Regulation of TPI1 Creates a Divergent Metabolic Liability between Human and Mouse Lung Adenocarcinoma [ Cancer Discov, 2023, 13(4):1002-1025] PubMed: 36715544
Glycolysis regulates KRAS plasma membrane localization and function through defined glycosphingolipids [ Nat Commun, 2023, 14(1):465] PubMed: 36709325
Mutant KRAS Drives Immune Evasion by Sensitizing Cytotoxic T-Cells to Activation-Induced Cell Death in Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(6):e2203757] PubMed: 36599679
Genotype-phenotype mapping of a patient-derived lung cancer organoid biobank identifies NKX2-1-defined Wnt dependency in lung adenocarcinoma [ Cell Rep, 2023, 42(3):112212] PubMed: 36870059

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.