INCB28060

C-Met inhibitor,ATP-competitive and novel CAS# 1029712-80-8

INCB28060

Catalog No. BCC3793----Order now to get a substantial discount!

Product Name & Size Price Stock
INCB28060: 5mg $58 In Stock
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Chemical structure

INCB28060

3D structure

Chemical Properties of INCB28060

Cas No. 1029712-80-8 SDF Download SDF
PubChem ID 25145656 Appearance Powder
Formula C23H17FN6O M.Wt 412.42
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Capmatinib; INC-280
Solubility H2O : 10 mg/mL (24.25 mM; Need ultrasonic)
DMSO : 3.33 mg/mL (8.07 mM; Need ultrasonic)
Chemical Name 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
SMILES CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
Standard InChIKey LIOLIMKSCNQPLV-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of INCB28060

DescriptionINCB28060 is a novel, ATP-competitive inhibitor of c-MET with an IC50 value of 0.13 nM.
Targetsc-MET    
IC500.13 nM     

Protocol

Cell Assay [1]
Optimal cell density used in the viability assay is predetermined for individual cell lines. To determine compound potency, cells are seeded into 96-well microplates at the appropriate density in media containing 1% to 2% FBS and supplemented with serial dilutions of INCB28060 in a final volume of 100 μL per well. After 72 hour incubation, 24 μL of CellTiter 96 AQueous One Solution is added to each well, and the plates are incubated for 2 hours in a 37°C incubator. The optical density is measured in the linear range using a microplate reader at 490 nm with wavelength correction at 650 nm. IC50 values are calculated using the GraphPad Prism Software[1].

Animal Administration [1]
Mice[1] Tumor-bearing mice are dosed orally, twice each day with 1, 3, 10, or 30 mg/kg of free base INCB28060 reconstituted in 5% DMAC in 0.5% methylcellulose for up to 2 weeks. Body weights are monitored throughout the study as a gross measure of toxicity/morbidity. Tumor growth inhibition, expressed in percent, is calculated using the formula: (1−[(volume (treated)/volume (vehicle)])×100.

References:
[1]. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

INCB28060 Dilution Calculator

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INCB28060 Molarity Calculator

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Preparing Stock Solutions of INCB28060

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4247 mL 12.1236 mL 24.2471 mL 48.4943 mL 60.6178 mL
5 mM 0.4849 mL 2.4247 mL 4.8494 mL 9.6989 mL 12.1236 mL
10 mM 0.2425 mL 1.2124 mL 2.4247 mL 4.8494 mL 6.0618 mL
50 mM 0.0485 mL 0.2425 mL 0.4849 mL 0.9699 mL 1.2124 mL
100 mM 0.0242 mL 0.1212 mL 0.2425 mL 0.4849 mL 0.6062 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on INCB28060

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.

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References on INCB28060

A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.[Pubmed:21918175]

Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

PURPOSE: The c-MET receptor tyrosine kinase plays important roles in the formation, progression, and dissemination of human cancer and presents an attractive therapeutic target. This study describes the preclinical characterization of INCB28060, a novel inhibitor of c-MET kinase. EXPERIMENTAL DESIGN: Studies were conducted using a series of in vitro and in vivo biochemical and biological experiments. RESULTS: INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, INCB28060 potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro. Oral dosing of INCB28060 results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition. In a further exploration of potential interactions between c-MET and other signaling pathways, we found that activated c-MET positively regulates the activity of epidermal growth factor receptors (EGFR) and HER-3, as well as expression of their ligands. These effects are reversed with INCB28060 treatment. Finally, we confirmed that circulating hepatocyte growth factor levels are significantly elevated in patients with various cancers. CONCLUSIONS: Activated c-MET has pleiotropic effects on multiple cancer-promoting signaling pathways and may play a critical role in driving tumor cell growth and survival. INCB28060 is a potent and selective c-MET kinase inhibitor that may have therapeutic potential in cancer treatment.

Description

Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib (INC280; INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity.

Keywords:

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