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ChemicalBook--->CAS DataBase List--->1637658-98-0

1637658-98-0

1637658-98-0 Structure

1637658-98-0 Structure
IdentificationBack Directory
[Name]

2H-1,4-Oxazino[3,2-c]quinolin-3(4H)-one, 9-[[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-a]pyridin-3-yl]thio]-4-methyl-
[CAS]

1637658-98-0
[Synonyms]

dalmelitinib
2H-1,4-Oxazino[3,2-c]quinolin-3(4H)-one, 9-[[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-a]pyridin-3-yl]thio]-4-methyl-
[Molecular Formula]

C22H16FN7O2S
[MOL File]

1637658-98-0.mol
[Molecular Weight]

461.47
Chemical PropertiesBack Directory
[density ]

1.61±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

2.94±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC)[1].
[in vivo]

Dalmelitinib (Compound 4 d, intragastric administration, 10-60 mg/kg) significantly inhibits the tumor growth in a dose-dependent manner in MKN-45 tumor xenograft nude mice[1].
Dalmelitinib (intragastric administration, 5 mg/kg for a single dose) shows a high plasma concentration, longer half-life and mean residence time, low clearance rates in BALB/c small nude mice[1].
Dalmelitinib shows a high level of No Observed Adverse Effect Level (NOAEL) in mice long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day)[1].

Animal Model:MKN-45 tumor xenograft nude mice[1]
Dosage:10, 30, 60 mg/kg
Administration:Intragastric administration
Result:Inhibited the tumor growth with the inhibitory rates of 29.5% (10 mg/kg), 34.2% (30 mg/kg), and 61.4% (60 mg/kg).
Animal Model:BALB/c small nude mice (pharmacokinetic assay)[1]
Dosage:5 mg/kg for a single dose
Administration:Intragastric administration
Result:Pharmacokinetic profile of Dalmelitinib (Compound 4 d)
Compound Cmax (ng/mL)AUC (ng/mL/h) t1/2 (h)MRT (h) CL/F (mL/min/kg)Vz/F
Dalmelitinib 86281224875.559.100.68327
[References]

[1] Junjun Zhao, et al. Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. Bioorg Med Chem. 2016 Aug 15;24(16):3483-93. DOI:10.1016/j.bmc.2016.05.057
1637658-98-0 suppliers list
Company Name: TargetMol Chemicals Inc.
Tel: +17819995354 , +17819995354
Website:
Company Name: Hebei Weite Medical Technology Co., Ltd  
Tel: 13180081292
Website: www.wetogethermed.com/
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
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