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Sotorasib

Catalog No. T8684   CAS 2296729-00-3
Synonyms: AMG-510

Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.

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Sotorasib Chemical Structure
Sotorasib, CAS 2296729-00-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 128.00
25 mg In stock $ 237.00
50 mg In stock $ 393.00
100 mg In stock $ 483.00
500 mg In stock $ 1,080.00
1 g In stock $ 1,430.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.88%
Purity: 99.36%
Purity: 99.25%
Purity: 98.91%
Purity: 98.91%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
In vitro METHODS: Twenty-two tumor cells were treated with Sotorasib (0-10 μM) for 72 h. Cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay kit.
RESULTS: Sotorasib impaired the growth of all KRAS G12C cell lines except SW1573, with IC50 values ranging from 0.004-0.032 μM. non-KRAS G12C cell lines were sensitive to Sotorasib, with an IC50 >7.5 μM. [1]
METHODS: KRAS G12C mutant tumor cells were treated with Sotorasib (100 nM) for 4-72 h, and the expression levels of target proteins were detected using Western Blot method.
RESULTS: Sotorasib rapidly inhibited KRAS downstream signaling, but p-ERK levels returned to 75% of the baseline level at 72 h. Sotorasib was also shown to rapidly inhibit KRAS downstream signaling. [2]
In vivo METHODS: To assay antitumor activity in vivo, Sotorasib (3-100 mg/kg) was orally administered once daily for four weeks to athymic nude mice bearing the human pancreatic cancer tumor MIA PaCa-2 T2 or the human lung cancer tumor NCI-H358.
RESULTS: Sotorasib significantly inhibited the growth of MIA PaCa-2 T2 and NCI-H358 tumors at all doses, and tumor regression was observed at higher doses. [1]
METHODS: To assay antitumor activity in vivo, Sotorasib (30 mg/kg in 0.5% sodium carboxymethylcellulose, administered by gavage once daily) and Cisplatin (4 mg/kg in 0.9% saline, intraperitoneally every two days) were administered to Balb/C nude mice harboring human lung cancer tumors.
RESULTS: Tumor shrinkage in the combination group was more than twice that of the single-administration group. [3]
Synonyms AMG-510
Molecular Weight 560.59
Formula C30H30F2N6O3
CAS No. 2296729-00-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (89.19 mM), sonification is recommended.

H2O: 33.33 mg/mL (59.46 mM), ultrasonic and adjust pH to 11 with NaOH

TargetMolReferences and Literature

1. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. 2. Ryan MB, et al. KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy. Cell Rep. 2022 Jun 21;39(12):110993. 3. Wu LL, et al. AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research. Discov Oncol. 2023 Jun 7;14(1):91.

TargetMolCitations

1. Yang N, Fan Z, Sun S, et al.Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.European Journal of Medicinal Chemistry.2023: 115857. 2. Yun S D, Scott E, Moghadamchargari Z, et al.2′-Deoxy Guanosine Nucleotides Alter the Biochemical Properties of Ras.Biochemistry.2023 3. Wu L L, Jiang W M, Liu Z Y, et al.AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research.Discover Oncology.2023, 14(1): 91. 4. Guo Y, Tian J, Guo Y, et al.Oncogenic KRAS effector USP13 promotes metastasis in non-small cell lung cancer through deubiquitinating β-catenin.Cell Reports.2023, 42(12).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Covalent Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Anti-Prostate Cancer Compound Library Anti-Pancreatic Cancer Compound Library Clinical Compound Library

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Keywords

Sotorasib 2296729-00-3 GPCR/G Protein MAPK Ras AMG510 KRAS covalent regression mutation Inhibitor G12C anti-tumour AMG-510 inhibit GDP-bound AMG 510 phosphorylation NSCLC inhibitor

 

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