Home>>Signaling Pathways>> Apoptosis>> Other Apoptosis>>INCB28060

INCB28060 Sale

(Synonyms: 卡马替尼; INC280; INCB28060) 目录号 : GC17866

An inhibitor of HGFR (c-Met)

INCB28060 Chemical Structure

Cas No.:1029712-80-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥494.00
现货
10mg
¥746.00
现货
50mg
¥2,205.00
现货
100mg
¥4,011.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment [1]:

Kinase assays

The assay buffer contained 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, 5mM DTT, pH 7.8. For HTS 0.8 μL of 5 mM of the test compounds dissolved in DMSO were dotted on 384-well plates. To measure IC50s the compound plate was prepared by 3-fold and 11-point serial dilutions. 0.8 μL of the compound in DMSO was transferred from the compound plate to the assay plate. Solutions of 8 nM unphosphorylated c-Met or 0.5 nM phosphorylated c-Met were prepared in assay buffer. A 1 mM stock solution of peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO was diluted to 1 μM in assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met). A 20 μL volume of enzyme solution was added to the appropriate wells in each plate and then 20 μL/well of substrate solution to initiate the reaction. The plate was protected from light and incubated at 25 °C for 90 min. The reaction was stopped by adding 20 μL of a solution containing 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC and 3 nM EU-Py20. The plate was incubated for 15-30 min at room temperature and HTRF (homogenous time resolved fluorescence) was measured on a Perkin Elmer Fusion α-FP instrument.

Cell experiment [2]:

Cell lines

Human cancer cell lines (SNU-5, SNU-1, U-87MG, 786-O, A549, H441, H596, H1437, H1993, BT474, A549, and HT-29), MKN-45 cell line, S114 cell line, Blood samples obtained from healthy volunteers and cancer patients

Preparation method

Limited solubility in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

IC50: 0.13 nM (c-MET), 72-hour

Applications

INCB28060 (IC50: 1 nM) inhibited human c-MET phosphorylation and c-MET–mediated signaling in the SNU-5 human gastric cancer cell line. INCB28060 inhibited SNU-5 viability or proliferation with an average IC50 value of 1.2 nM. INCB28060 (2 nM) prevented HGF-stimulated H441 cell migration. INCB28060 exhibited strong antitumor activity in c-MET-dependent tumor models. INCB28060 exhibited picomolar enzymatic potency and was highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. INCB28060 (24 hours) potently inhibited c-MET-dependent tumor cell proliferation and migration and effectively induced apoptosis.

Animal experiment [2]:

Animal models

Female Balb/c nu/nu mice (Charles River) subcutaneously injected with S114 tumor cells or U-87MG glioblastoma tumor cells

Dosage form

0.03, 0.1, 0.3, 1, 3, or 10 mg/kg

Application

Oral dosing of INCB28060 resulted in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models. INCB28060 was well tolerated at doses that achieve complete tumor inhibition. Once daily dosing of 10 mg/kg INCB28060 resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Behshad E, Klabe R M, Margulis A, et al. Phosphorylation state-dependent high throughput screening of the c-MET kinase[J]. Current chemical genomics, 2010, 4: 27.

[2]. Liu X, Wang Q, Yang G, et al. A novel kinase inhibitor INCB28060 blocks c-MET-dependent signaling, neoplastic activities, and crosstalk with EGFR and HER-3[J]. Clinical Cancer Research, 2011: clincanres. 1157.2011.

产品描述

INCB28060, also known as Capmatinib and INC280, is a novel and ATP-competitive inhibitor of c-Met with IC50 of 0.13 nM.

c-Met, also named as hepatocyte growth factor receptor (HGFR) is a receptor tyrosine kinase that is essential for embryonic development and would healing. In many tumor cells, this molecular is overexpressed or mutated and was found to play important roles in tumor cell proliferation, survival, invasion, metastasis and angiogenesis.

In vitro, INCB28060 treatment effectively inhibited activation of c-MET and signaling in cancer cells. As a result, INCB28060 blocked cell proliferation of varying cell lines such as SNU-5 and S114. The cell migration of U-87MG and H441 cells were also highly inhibited1.

The role of c-met was studied using this inhibitor in mouse model. Oral administration of INCB28060 leads to inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models. Therefore, INCB28060 has the therapeutic potential in cancer treatment 1.

Reference:
1.   Liu X, Wang Q, Yang G, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011;17(22):7127-7138.

Chemical Properties

Cas No. 1029712-80-8 SDF
别名 卡马替尼; INC280; INCB28060
化学名 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
Canonical SMILES CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
分子式 C23H17FN6O 分子量 412.42
溶解度 ≥ 5.15mg/mL in DMSO with gentle warming 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.4247 mL 12.1236 mL 24.2471 mL
5 mM 0.4849 mL 2.4247 mL 4.8494 mL
10 mM 0.2425 mL 1.2124 mL 2.4247 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置