Sotorasib (AMG510)

製品コードS8830 バッチS883003

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C30H30F2N6O3
分子量 560.59 CAS No. 2296729-00-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (178.38 mM)
Ethanol 8 mg/mL (14.27 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.

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生物活性

製品説明 Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HBEC30KT cells
濃度 1 uM
反応時間 48 h
実験の流れ

Cells were treated with AMG-510 (1 μM) or DMSO for 48 h.
動物実験 動物モデル Female ICR-SCID mice
投薬量 100 mg/kg
投与方法 o.g.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。