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.
Synthesis
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
Raw materials
Preparation Products
Capmatinib Suppliers
- Tel
- 0512-68780025 18962125825
- sales@ryanchem.com
- Country
- China
- ProdList
- 167
- Advantage
- 62
- Tel
- 0371-0371-55629727 13323845623
- Fax
- 037155629727
- 2885676761@qq.com
- Country
- China
- ProdList
- 10110
- Advantage
- 58
- Tel
- 13606124132;13656121842
- luyan0021@163.com
- Country
- China
- ProdList
- 235
- Advantage
- 58
- Tel
- 13302022156
- Fax
- -
- 3506745780@qq.com
- Country
- China
- ProdList
- 163
- Advantage
- 58
- Tel
- 0886-1313565-2018 18662190408
- 275443226@qq.com
- Country
- China
- ProdList
- 148
- Advantage
- 58
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6003
- Advantage
- 61
- Tel
- 0531-88811783
- Fax
- +86 (531) 55696010 QQ 1762738062
- sales@trio-pharmatech.com
- Country
- China
- ProdList
- 1856
- Advantage
- 62
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4747
- Advantage
- 58
- Tel
- 021-61551611 13296011611
- Fax
- ＋86 21-50676805
- contact@trustwe.com
- Country
- China
- ProdList
- 9895
- Advantage
- 58
- Tel
- 021-58170097
- info@topbiochem.com
- Country
- China
- ProdList
- 9510
- Advantage
- 58
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
- Fax
- +86-27-87599188
- Country
- China
- ProdList
- 1493
- Advantage
- 55
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 400-6206333 13167063860
- Fax
- 021-50323701
- anhua.mao@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- +86 13671938079
- Fax
- +86-021-50829787
- Country
- China
- ProdList
- 39
- Advantage
- 55
- Tel
- +86-21-38682181 15900741819
- Fax
- +86-21-38682181
- Country
- China
- ProdList
- 282
- Advantage
- 55
- Tel
- sales@witofly.com
- Country
- China
- ProdList
- 2864
- Advantage
- 52
- Tel
- 020-39119399 18927568969
- Fax
- 020-39119999
- isunpharm@qq.com
- Country
- China
- ProdList
- 4720
- Advantage
- 55
- Tel
- 025-57798810
- Fax
- 025-57019371
- sales@sunlidabio.com
- Country
- China
- ProdList
- 3239
- Advantage
- 55
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7783
- Advantage
- 58
- Tel
- 86-21-50700185 13764109623
- Fax
- 86-21-50700185
- sale@inyelchem.com
- Country
- China
- ProdList
- 178
- Advantage
- 55
- Tel
- 0531-85828981
- Fax
- +86-531-85806006
- 864598798@qq.com
- Country
- China
- ProdList
- 588
- Advantage
- 58
- Tel
- 027-84888681 18086046872
- Fax
- 027-84888682
- hhdpharm@hotmail.com
- Country
- China
- ProdList
- 105
- Advantage
- 55
- Tel
- 400-0066400 13621662912
- Fax
- 021-55660885
- 422131432@qq.com
- Country
- China
- ProdList
- 9979
- Advantage
- 55
- Tel
- 027-87465837 19945049750
- Fax
- 027-8777-2287
- sales@finetechnology-ind.com
- Country
- China
- ProdList
- 9637
- Advantage
- 58
- Tel
- 0898-66518050 13307521111
- Fax
- +86 (898) 6677-5768
- mfy001@hnmfy.com
- Country
- China
- ProdList
- 85
- Advantage
- 60
- Tel
- 15221275939
- Fax
- 021-50706099
- shenlinxing@macklin.cn
- Country
- China
- ProdList
- 15873
- Advantage
- 55
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- +86 (21) 61124340
- Fax
- +86 (21) 6129-4103
- Country
- China
- ProdList
- 9756
- Advantage
- 58
- Tel
- 400-026-9899
- Fax
- +86-731-86905278
- Country
- China
- ProdList
- 71
- Advantage
- 50
- Tel
- 027-59599241 18871490274
- Fax
- 027-59599241
- 1400878000@qq.com
- Country
- China
- ProdList
- 9858
- Advantage
- 58
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- 021-50426030 13856289449
- Fax
- 021-50426030
- 2630597085@qq.com
- Country
- China
- ProdList
- 1889
- Advantage
- 55
- Tel
- +86-371-55216238
- Fax
- +86-371-86615086
- Country
- China
- ProdList
- 286
- Advantage
- 60
- Tel
- 021-57898186
- Fax
- 021-37699262
- Country
- China
- ProdList
- 449
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 984
- Advantage
- 55
- Tel
- 18607101326 15172504745
- Fax
- +86-27-84254680
- aileen@chemfaces.com
- Country
- China
- ProdList
- 6905
- Advantage
- 55
- Tel
- 0514-80939770 13773367191
- Fax
- 0514-82664689
- yzqyyykj@163.com
- Country
- China
- ProdList
- 252
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 316
- Advantage
- 55
- Tel
- 021-26018599
- Country
- China
- ProdList
- 270
- Advantage
- 56
- Tel
- 021-5068 3667/17749785980/1029026415; 17749785980
- Fax
- 021-50683667
- 1029026415@qq.com
- Country
- China
- ProdList
- 3397
- Advantage
- 58
- Tel
- 0512-66242155 13382105697
- Fax
- 0512-66242155
- sedswkj@163.com
- Country
- China
- ProdList
- 39
- Advantage
- 55
- Tel
- 021-58088081 Q2635253576
- Fax
- QQ3382968513
- hailey@shsendpharm.com
- Country
- China
- ProdList
- 2081
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 6687
- Advantage
- 55
- Tel
- +86-400-851-9921
- Fax
- +86-10-82826195
- sales@pharmacodia.com
- Country
- China
- ProdList
- 2317
- Advantage
- 55
- Tel
- +86-010-60279497 +86-15646567669
- Fax
- 010-60279497
- sales01@cooperate-pharm.com
- Country
- China
- ProdList
- 137
- Advantage
- 58
- Tel
- 0931-8235634 13321316780
- Fax
- +86(931) 4873122
- 1455540579@qq.com
- Country
- China
- ProdList
- 958
- Advantage
- 55
- Tel
- 021-31761238 13167072949
- Fax
- 021-31761238
- 3146446224@qq.com
- Country
- China
- ProdList
- 1379
- Advantage
- 55
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 71826
- Advantage
- 60
View Lastest Price from Capmatinib manufacturers
- 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/mg
- Min. Order
- 10mg
- Purity
- 98
- Supply Ability
- 100000
- Release date
- 2025-02-11
- 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