Glumetinib(Synonyms: SCC244)

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Glumetinib (Synonyms: SCC244) 纯度: 98.15%

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。

Glumetinib(Synonyms: SCC244)

Glumetinib Chemical Structure

CAS No. : 1642581-63-2

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10 mM * 1 mL in DMSO ￥1365 In-stock
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10 mg ￥2100 In-stock
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100 mg ￥8650 In-stock
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生物活性

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 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[1].

IC50 & Target

IC50: 0.42 nM (c-Met kinase)[1]
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[1].
Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells
Concentration: 0-10 nM
Incubation Time: 72 hours
Result: Specifically and potently inhibited proliferation of c-Met–addicted human cancer cells (IC50 ranging 0.5 to 2.45 nM for EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells ).

Cell Cycle Analysis[1]

Cell Line: EBC-1 and MKN-45 cells
Concentration: 0-50 nM
Incubation Time: 24 hours
Result: Consistently induced G1–S cell-cycle arrest.

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[1].
Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (4-6 weeks old) (MKN-45 model)[1]
Dosage: 10, 5, 2.5 mg/kg
Administration: P.o.; once daily for 2-3 weeks
Result: Significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively.

Clinical Trial

分子量

459.48

Formula

C21H17N9O2S
CAS 号

1642581-63-2
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1764 mL 10.8819 mL 21.7637 mL
5 mM 0.4353 mL 2.1764 mL 4.3527 mL
10 mM 0.2176 mL 1.0882 mL 2.1764 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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