1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. Glumetinib

Glumetinib  (Synonyms: Gumarontinib; SCC244)

目录号: HY-116000 纯度: 99.92%
COA 产品使用指南

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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Glumetinib Chemical Structure

Glumetinib Chemical Structure

CAS No. : 1642581-63-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1365
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1 mg ¥613
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5 mg ¥1350
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10 mg ¥2100
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50 mg ¥5350
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100 mg ¥8650
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
性状

固体

颜色

White to off-white

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 中的溶解度 : 41.67 mg/mL (90.69 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Glumetinib 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1764 mL 10.8819 mL 21.7637 mL 54.4093 mL
5 mM 0.4353 mL 2.1764 mL 4.3527 mL 10.8819 mL
10 mM 0.2176 mL 1.0882 mL 2.1764 mL 5.4409 mL
15 mM 0.1451 mL 0.7255 mL 1.4509 mL 3.6273 mL
20 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7205 mL
25 mM 0.0871 mL 0.4353 mL 0.8705 mL 2.1764 mL
30 mM 0.0725 mL 0.3627 mL 0.7255 mL 1.8136 mL
40 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
50 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Glumetinib
目录号:
HY-116000
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