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ChemicalBook >> CAS DataBase List >>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-

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 No.
1637658-98-0
Chemical 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-
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-
CBNumber:
CB012020481
Molecular Formula:
C22H16FN7O2S
Molecular Weight:
461.47
MDL Number:
MOL File:
1637658-98-0.mol
Last updated:2025-04-29 09:03:59

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- Properties

Density 1.61±0.1 g/cm3(Predicted)
form Solid
pka 2.94±0.20(Predicted)
color White to off-white
FDA UNII 4SP7R879Y5

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- Chemical Properties,Uses,Production

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

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- Preparation Products And Raw materials

Raw materials

Preparation Products

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- Suppliers

Global( 3)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc.
+17819995354 marketing@targetmol.com United States 19927 58
Hebei Weite Medical Technology Co., Ltd 13180081292 contact@wetogethermed.com China 7977 58
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 24803 58

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Dalmelitinib pictures 2025-04-29 Dalmelitinib
1637658-98-0
US $3520.00-2785.00 / mg 10g TargetMol Chemicals Inc.
  • Dalmelitinib pictures
  • Dalmelitinib
    1637658-98-0
  • US $3520.00-2785.00 / mg
  • TargetMol Chemicals Inc.
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- dalmelitinib 1637658-98-0 C22H16FN7O2S