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
- Molecular Weight:
- 412.42
- MDL Number:
- MFCD18633285
- MOL File:
- 1029712-80-8.mol
- MSDS File:
- SDS
| Product description | Number | Pack Size | Price |
| INCB 28060 ≥98% | 20056 | 5mg | $88 |
| INCB 28060 ≥98% | 20056 | 10mg | $157 |
| INCB 28060 ≥98% | 20056 | 50mg | $647 |
| Capmatinib | FF40658 | 500mg | $800 |
| Capmatinib 99.92% | CS-1541 | 200mg | $190 |
| More product size | |||
| 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 |
| FDA UNII | TY34L4F9OZ |
| ATC code | L01EX17 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Capmatinib price More Price(28)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 20056 | INCB 28060 ≥98% | 1029712-80-8 | 5mg | $88 | 2024-03-01 | Buy |
| Cayman Chemical | 20056 | INCB 28060 ≥98% | 1029712-80-8 | 10mg | $157 | 2024-03-01 | Buy |
| Cayman Chemical | 20056 | INCB 28060 ≥98% | 1029712-80-8 | 50mg | $647 | 2024-03-01 | Buy |
| Biosynth Carbosynth | FF40658 | Capmatinib | 1029712-80-8 | 500mg | $800 | 2021-12-16 | Buy |
| ChemScene | CS-1541 | Capmatinib 99.92% | 1029712-80-8 | 200mg | $190 | 2021-12-16 | Buy |
Capmatinib Chemical Properties,Uses,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
Capmatinib is a competitive inhibitor with very potent and selective activity against MET compared to other kinases.
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.
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.
Synthesis
![2-fluoro-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzoicacid](/CAS/20180702/GIF/1029714-88-2.gif)
1029714-88-2
74-89-5
1029712-80-8
Example 20 Synthesis of 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide (15): 2-fluoro-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzoic acid (14, 331.4 g, 0.914 mol, 1.0 eq.) and (benzotriazol-1-yloxy)tripyrrolidinylphosphonium hexafluorophosphate (PyBOP, 570 g, 1.1 mol, 1.2 eq.) were dissolved in N,N-dimethylformamide (DMF, 3700 mL). To this solution, a tetrahydrofuran solution of 2M methylamine (1830 mL, 3.656 mol, 4.0 eq.) was slowly added for 15 min at room temperature. The reaction temperature was raised to 30 °C during the addition and the reaction mixture became homogeneous. Subsequently, triethylamine (TEA, 382 mL, 2.742 mol, 3.0 eq.) was added to the reaction mixture and the reaction mixture was stirred for 2-4 h at room temperature. The progress of the reaction was monitored by LC/MS and after confirming the completion of the coupling reaction, water (950 mL) was added to the reaction mixture. The resulting suspension was cooled to 0-5 °C in an ice bath and stirred at this temperature for 30 min. The solid was collected by filtration and washed with water (200 mL). The wet solid filter cake was suspended in a solvent mixture of water and acetonitrile (1:1 v/v, 2000 mL) and stirred for 1 hour at room temperature. The solid was collected by filtration, washed sequentially with water and acetonitrile, and then dried to constant weight in a vacuum oven at 40-45 °C to afford 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide (15, 322 g, 85.4% yield) as a yellow to bright yellow powder.
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhengzhou Anhuida Chemical Co., Ltd | +8615903659408 | admin@ahdchem.com | China | 286 | 58 |
| Suzhou Ryan Pharmachem Technology Co.,Ltd. | +86-512-68780025 | sales@ryanchem.com | China | 169 | 58 |
| Suzhou ARTK Medchem Co., Ltd. | +8618118463618 | sales1@artkmedchem.com | China | 39020 | 58 |
| shandong perfect biotechnology co.ltd | +86-53169958659 +86-13153181156 | sales@sdperfect.com | China | 294 | 58 |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 | sales@sjar-tech.com | China | 529 | 58 |
| Moxin Chemicals | +86-17320513646 +8617320513646 | anna@molcoo.com | China | 10000 | 58 |
| Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 | CHINA | 115 | 55 | |
| Nanjing Finetech Chemical Co., Ltd. | 025-85710122 17714198479 | sales@fine-chemtech.com | CHINA | 885 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Shanghai Arbor Chemical Co., Ltd. | 021-60451682 | act@arborchemical.com | CHINA | 904 | 58 |
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View Lastest Price from Capmatinib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-04-23 | Capmatinib
1029712-80-8
|
US $0.00 / g | 1g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | |
 |
2026-04-22 | Capmatinib
1029712-80-8
|
US $43.00-75.00 / mg | 99.98% | 10g | TargetMol Chemicals Inc. | ||
 |
2026-03-27 | Capmatinib
1029712-80-8
|
US $0.00 / g | 1g | 98% HPLC | 1KG | shandong perfect biotechnology co.ltd |
-
- Capmatinib
1029712-80-8
- US $0.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
-
- Capmatinib
1029712-80-8
- US $43.00-75.00 / mg
- 99.98%
- TargetMol Chemicals Inc.
-
- Capmatinib
1029712-80-8
- US $0.00 / g
- 98% HPLC
- shandong perfect biotechnology co.ltd
