产品
编 号：F746417
分子式：C22H16FN7O2S
分子量：461.47
分子式：C22H16FN7O2S
分子量：461.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1637658-98-0
产品详情
生物活性：
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).
体内研究：
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.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.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).Animal Model:MKN-45 tumor xenograft nude mice
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)
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
体外研究：
Dalmelitinib (Compound 4 d) binds to the ATP-binding region of c-Met kinase, and shows slective inhibitory activity against c-Met with an IC50 value of 2.9 nM.Dalmelitinib (0-1 μM approximately, 3 days) inhibits cell proliferation in various c-Met oncogene amplification cancer cell lines, with IC50 values ranging from 6 nM to 33 nM.Dalmelitinib (0.1-1 μM, 6-24 h) significantly induces the phosphorylation of the tyrosine kinases (MET), partially or completely inhibits the downstream phosphorylation of ERK and AKT in HCCLM3 cells.
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).
体内研究：
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.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.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).Animal Model:MKN-45 tumor xenograft nude mice
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)
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
体外研究：
Dalmelitinib (Compound 4 d) binds to the ATP-binding region of c-Met kinase, and shows slective inhibitory activity against c-Met with an IC50 value of 2.9 nM.Dalmelitinib (0-1 μM approximately, 3 days) inhibits cell proliferation in various c-Met oncogene amplification cancer cell lines, with IC50 values ranging from 6 nM to 33 nM.Dalmelitinib (0.1-1 μM, 6-24 h) significantly induces the phosphorylation of the tyrosine kinases (MET), partially or completely inhibits the downstream phosphorylation of ERK and AKT in HCCLM3 cells.
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