AMG 510 (Sotorasib)

製品コードS8830 バッチS883008

化学情報

	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	12.5 mg/mL (22.29 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Sotorasib (AMG510)は、潜在的な抗腫瘍活性を持つ強力なKRAS G12C共有結合阻害剤です。このAMG510はキラル化合物です。
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 tumor models, Sotorasib (AMG510) 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, it is capable of inducing tumor regression in mouse models of KRASG12C cancer.

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 Sotorasib (AMG510) (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.

参考

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/

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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：

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

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。