Glumetinib Gumarontinib; SCC244|cas:1642581-63-2|西域试剂

Glumetinib Gumarontinib; SCC244,98.30%

产品编号：Bellancom-116000| CAS NO：1642581-63-2| 分子式：C₂₁H₁₇N₉O₂S| 分子量：459.48

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货号	价格	库存与货期
Bellancom-116000	￥1350.00	杭州北京（现货）
Bellancom-116000	￥2100.00	杭州北京（现货）
Bellancom-116000	￥5350.00	杭州北京（现货）
Bellancom-116000	￥8650.00	杭州北京（现货）

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Glumetinib Gumarontinib; SCC244

产品介绍

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 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)
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.

体内研究

西域 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)
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.

体内研究

西域 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)
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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式