Sotorasib (AMG510)

目录号：S8830 批次号：S883005

化学数据

	别名	N/A	储存条件 (自收到货起)	3年 -20°C 粉状
	化学式	C₃₀H₃₀F₂N₆O₃
	分子量	560.59	CAS号	2296729-00-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (178.38 mM)
		Water	Insoluble
		Ethanol	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.

制备储备液

生物活性

产品描述

Sotorasib (AMG510) 是有效的KRAS G12C共价抑制剂，具有潜在的抗肿瘤活性。该AMG510是手性化合物。

靶点

K-Ras(G12C) ^[1]

体外研究

AMG 510抑制SOS1催化的重组突变体KRAS (G12C/C118A)的核苷酸交换，但对单突变KRAS (C118A)影响甚微。AMG 510选择性地降低含KRAS p.G12C突变的细胞系生存活力，而对含其它KRAS突变的细胞系无影响^[1]。

体内研究

在临床前肿瘤模型中，AMG 510可快速地以不可逆方式结合KRAS (G12C)，持久地抑制MAPK信号通路。对含KRAS(G12C)突变的小鼠肿瘤模型通过口服途径单次给药，AMG 510能够诱导肿瘤消退^[2]。

参考文献

[4] Khan HY, et al. Cancer Res Commun. 2022 May;2(5):342-352.

+ 展开

Sotorasib (AMG510)在文献中得到引用

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

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20°C，抑制剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

如果需要长期保存，请于零下二十度低温保存。禁止用于人体及治疗！

退换货政策

Selleck提供宽松的退换货承诺，努力为您营造最优的购物体验。每个订单Selleck只提供一次退换货服务，为了确保您的权益，请您仔细阅读以下内容：

1. 请在返还样品之前事先与我们取得联系，以确保产品是直接向我们或者当地代理商购买的；

2. 自收到货物起七天内，如因运输过程有问题或其他任何问题，您可以提出退换货要求；自收到货物起365天内，如因产品质量有问题，您可以提出退换货要求。

3. 请使用我们的快递账号进行退换货，您无需为此承担任何费用。

4. 如您已收到由Selleck开具的发票，则办理退货或订单金额发生变更的换货时，请将发票随商品一同返还给Selleck。请您妥善保管发票，如发票丢失，将无法办理退换货手续。