Glumetinib|1642581-63-2|(Gumarontinib; SCC244)-陌孚医药/Medlife

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Glumetinib (Synonyms: Gumarontinib; SCC244)

目录号: PL02282 纯度: ≥98%

CAS No. :1642581-63-2

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中文名称	Glumetinib
英文名称	Glumetinib
英文别名	Glumetinib;7JTT036WGX;SCC244;BCP31155;s8676;6-(1-Methyl-1H-pyrazol-4-yl)-1-((6-(1-methyl-1H-pyrazol-4-yl)imidazo(1,2-a)pyridin-3-yl)sulfonyl)-1H-pyrazolo(4,3-b)pyridine
Cas No.	1642581-63-2
分子式	C₂₁H₁₇N₉O₂S
分子量	459.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Glumetinib (SCC244) 是一种高选择性、口服生物利用度、ATP 竞争性 c-Met 抑制剂，IC₅₀ 为0.42 nM。Glumetinib 对 c-Met 的选择性超过 312 种激酶，包括 c-Met 家族成员 RON 和高度同源的激酶 Axl、Mer、TyrO3。Glumetinib 具有抗肿瘤活性。

生物活性

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC 50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.

性状

Solid

IC50 & Target[1][2]

IC50: 0.42 nM (c-Met kinase)

体外研究(In Vitro)

Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.
Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

体内研究(In Vivo)

Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.
Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762.

溶解度数据	In Vitro: DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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