产品
编 号：F038494
分子式：C18H18N4O2
分子量：322.36
分子式：C18H18N4O2
分子量：322.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 1111556-37-6
产品详情
生物活性：
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
体内研究：
Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis.?Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice.Animal Model:Male DBA/1 mice (CIA arthritis model)
Dosage:50 mg/kg
Administration:Intraperitoneally; daily from days 18-36
Result:Showed a reduction in clinical arthritic score compared to vehicle control.
Animal Model:Female NSG mice (8 weeks old)
Dosage:50 mg/kg
Administration:Oral gavage; daily until 17 days
Result:Slowed tumor growth and reduced tumor size/weight.
体外研究：
Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells.?Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65.?Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria.?Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs.
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
体内研究：
Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis.?Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice.Animal Model:Male DBA/1 mice (CIA arthritis model)
Dosage:50 mg/kg
Administration:Intraperitoneally; daily from days 18-36
Result:Showed a reduction in clinical arthritic score compared to vehicle control.
Animal Model:Female NSG mice (8 weeks old)
Dosage:50 mg/kg
Administration:Oral gavage; daily until 17 days
Result:Slowed tumor growth and reduced tumor size/weight.
体外研究：
Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells.?Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65.?Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria.?Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs.
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