产品
编 号：F314440
分子式：C27H30ClFN4O3
分子量：513
分子式：C27H30ClFN4O3
分子量：513
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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2mg
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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: 309913-83-5
产品详情
生物活性：
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
体内研究：
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination.Animal Model:Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)
Dosage:P.o.; twice daily orally for 14 days
Administration:10, 30, 90 mg/kg
Result:Dose-dependently reduced tumor growth.
体外研究：
Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.Talmapimod inhibits LPS-induced TNF-a production in human whole blood.Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
体内研究：
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination.Animal Model:Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)
Dosage:P.o.; twice daily orally for 14 days
Administration:10, 30, 90 mg/kg
Result:Dose-dependently reduced tumor growth.
体外研究：
Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.Talmapimod inhibits LPS-induced TNF-a production in human whole blood.Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
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