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
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)
|
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
Supplier | Tel | 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 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Hebei Weite Medical Technology Co., Ltd | 58 |
TargetMol Chemicals Inc. | 58 |
View Lastest Price from 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- manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2025-04-29 | Dalmelitinib
1637658-98-0
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US $3520.00-2785.00 / mg | 10g | TargetMol Chemicals Inc. |
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- Dalmelitinib
1637658-98-0
- US $3520.00-2785.00 / mg
- TargetMol Chemicals Inc.