Glumetinib - CAS:1642581-63-2

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Glumetinib (Synonyms:SCC244)

目录号 : KM5495 CAS No. : 1642581-63-2 纯度 : 98%

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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。

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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.

体外研究

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.

Cell Proliferation Assay

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

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

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.

Animal Model:	Female nude mice (4-6 weeks old) (MKN-45 model)
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.

分子式

C₂₁H₁₇N₉O₂S

分子量

459.48

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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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