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1029712-80-8 1865733-40-9
1029714-89-3 1197376-85-4

1029712-80-8

1029712-80-8 structure
1029712-80-8 structure
  • Name: Capmatinib (INCB28060)
  • Chemical Name: 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
  • CAS Number: 1029712-80-8
  • Molecular Formula: C23H17FN6O
  • Molecular Weight: 412.419
  • Catalog: Biochemical Inhibitor Protein tyrosine kinase
  • Create Date: 2018-05-28 08:00:00
  • Modify Date: 2024-01-09 00:13:19
  • Capmatinib (INCB28060) is a potent and selective c-MET kinase inhibitor. Capmatinib (INCB28060) inhibits c-MET kinase activity with an average IC50 of 0.13 nM.
Name 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
Synonyms 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazolo[1,2-b][1,2,4]triazin-2-yl]benzamide
cc-219
Benzamide
Capmatinib
QC-7530
UNII-TY34L4F9OZ
2-fluoro-N-methyl-4-[(7-quinolin-6-ylmethyl)imidazo[1,2-b]triazin-2-yl]benzamide
2-Fluoro-N-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
INC-280
2-fluoro-N-methyl-4-{7-[(quinolin-6-yl)methyl]imidazo[1,2- b][1,2,4]triazin-2-yl}benzamide
INCB28060
2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide
Description Capmatinib (INCB28060) is a potent and selective c-MET kinase inhibitor. Capmatinib (INCB28060) inhibits c-MET kinase activity with an average IC50 of 0.13 nM.
Related Catalog
Target

IC50: 0.13 nM (c-MET)[1]
In Vitro Capmatinib (INCB28060) inhibits c-MET phosphorylation with an IC50 value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%. Capmatinib (INCB28060) inhibits SNU-5 viability or proliferation with an average IC50 value of 1.2 nM and a calculated IC90 value of 4.6 nM Capmatinib (INCB28060) prevents HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM. Again, there is little cell migration at a concentration of 16 nM Capmatinib (INCB28060). Capmatinib (INCB28060) potently and specifically inhibits c-MET enzyme activity, c-MET-mediated signal transduction, and the c-MET-dependent neoplastic phenotype of tumor cells. Capmatinib (INCB28060) exhibits strong antitumor activity in c-MET-dependent tumor models at well-tolerated doses. Capmatinib (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. Capmatinib (INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis[1].
In Vivo Oral dosing of Capmatinib (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. Furthermore, once daily dosing of 10 mg/kg Capmatinib (INCB28060) results in partial regressions in 6 of 10 U-87MG tumor-bearing mice. It is noted that in both S114 and U-87MG models, tumor growth inhibition increases with increased exposure of the compound and that tumor regressions could only be achieved when the compound exposure consistently exceeded 90% of c-MET inhibition. In these studies, Capmatinib (INCB28060) is well tolerated at all doses during the treatment periods, with no evidence of overt toxicity or weight loss[1].
Cell Assay 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 Capmatinib (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 Admin Mice[1] Tumor-bearing mice are dosed orally, twice each day with 1, 3, 10, or 30 mg/kg of free base Capmatinib (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.
Density 1.4±0.1 g/cm3
Molecular Formula C23H17FN6O
Molecular Weight 412.419
Exact Mass 412.144775
PSA 88.56000
LogP -0.12
Index of Refraction 1.717
Storage condition 2~8℃
Hazard Codes Xi
1029714-88-2 structure

1029714-88-2
74-89-5 structure

74-89-5

~84%

1029712-80-8 structure

1029712-80-8
Literature: Weng, Lingkai; Qiao, Lei; Zhou, Jiacheng; Liu, Pingli; Pan, Yongchun Patent: US2009/291956 A1, 2009 ; Location in patent: Page/Page column 24-25 ;
Precursor  1

DownStream  0


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