Capmatinib
MET small molecule inhibitor Originator- Product Name
- Capmatinib
- CAS No.
- 1029712-80-8
- Chemical Name
- Capmatinib
- Synonyms
- INC280;INCB28060;INC28060;2-Fluoro-N-Methyl-4-(7-quinolin-6-ylMethyl-iMidazo[1,2-b][1,2,4] triazin-2-yl)-benzaMide;NC280;CS-192;INCB028060;NVP-INC280;CapMatinib;Karma for,
- CBNumber
- CB92574678
- Molecular Formula
- C23H17FN6O
- Formula Weight
- 412.42
- MOL File
- 1029712-80-8.mol
Capmatinib Property
- Melting point:
- >250°C (dec.)
- Density
- 1.40
- vapor pressure
- 0-0Pa at 20-25℃
- storage temp.
- -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 13.82±0.46(Predicted)
- form
- Solid
- color
- Pale Yellow to Light Yellow
- 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)
- InChIKey
- LIOLIMKSCNQPLV-UHFFFAOYSA-N
- SMILES
- C(NC)(=O)C1=CC=C(C2=NN3C(CC4=CC=C5C(=C4)C=CC=N5)=CN=C3N=C2)C=C1F
- LogP
- 1.6-2.2 at 35℃ and pH7-9
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 20056
- Product name
- INCB 28060
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $88
- Updated
- 2024/03/01
- Product number
- 20056
- Product name
- INCB 28060
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $157
- Updated
- 2024/03/01
- Product number
- 20056
- Product name
- INCB 28060
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $647
- Updated
- 2024/03/01
- Product number
- FF40658
- Product name
- Capmatinib
- Packaging
- 500mg
- Price
- $800
- Updated
- 2021/12/16
- Product number
- CS-1541
- Product name
- Capmatinib
- Purity
- 99.92%
- Packaging
- 200mg
- Price
- $190
- Updated
- 2021/12/16
Capmatinib Chemical Properties,Usage,Production
MET small molecule inhibitor
Capmatinib(Synonyms: INC280; INCB28060) is a competitive inhibitor with very potent and selective activity against MET compared to other kinases. It has been shown in vitro that cell lines made resistant to erlotinib, an EGFR inhibitor, could be resensitized after capmatinib treatment. Results from a phase Ib/II study of patients with EGFR-mutated, MET-dysregulated NSCLC have shown promising responses to a combination of capmatinib and gefitinib (EGFR TKI) following disease progression from an only EGFR TKI treatment regimen. Recommended phase II dose was determined to be capmatinib 400 mg twice/day and gefitinib 250 mg once/day. Most common adverse events were nausea, peripheral edema, decreased appetite, rash, and increased amylase and lipase levels.
Originator
Novartis
Description
INCB 28060 is an inhibitor of heptatocyte growth factor receptor (HGFR, also known as c-Met), potently blocking in vitro kinase activity (IC50 = 0.13 nM) as well as constitutive or HGF-stimulated activity in cells (IC50 values range from 0.3 to 1.1 nM). It blocks cell proliferation and migration or induces apoptosis in different types of cancer cells. INCB 28060 is orally bioavailable and inhibits the growth of HGFR-dependent tumors in mice. It also improves efficacy of gemcitabine in a mouse pancreatic cancer model and reduces migration and adhesion in ovarian cancer cell models.
Description
Capmatinib is a competitive inhibitor with very potent and selective activity against MET compared to other kinases.
Uses
2-Fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide is used in the preparation of a combination formulation with allosteric SHP2 inhibitor TNO155. Used in treatment of non-small cell lung cancer with specific mutations (those that lead to mesenchymal-epithelial transition or MET exon 14 skipping).
brand name
Tabrecta
General Description
Class: receptor tyrosine kinase; Treatment: NSCLC with METex14; Other name: INCB28060; Oral bioavailability >70%; Elimination half-life = 7.8 h; Protein binding = 96%
Side effects
Most common adverse events were nausea, peripheral edema, decreased appetite, rash, and increased amylase and lipase levels.
in vitro
It has been shown in vitro that cell lines made resistant to erlotinib, an EGFR inhibitor, could be resensitized after capmatinib treatment. Results from a phase Ib/II study of patients with EGFR-mutated, MET-dysregulated NSCLC have shown promising responses to a combination of capmatinib and gefitinib (EGFR TKI) following disease progression from an only EGFR TKI treatment regimen. Recommended phase II dose was determined to be capmatinib 400 mg twice/day and gefitinib 250 mg once/day.
target
c-MET
References
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.
Capmatinib Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Capmatinib manufacturers
- Product
- Capmatinib 1029712-80-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-10-14
- Product
- Capmatinib 1029712-80-8
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- ＞99% by HPLC
- Supply Ability
- 10kg/month
- Release date
- 2023-07-22
- Product
- Capmatinib 1029712-80-8
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%，single impurity＜0.1
- Supply Ability
- 1 ton
- Release date
- 2023-12-21