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编 号：F314443
分子式：C27H31Cl2FN4O3
分子量：549.46
分子式：C27H31Cl2FN4O3
分子量：549.46
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CAS No: 309915-12-6
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生物活性：
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride 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：
Talmapimod hydrochloride (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:10, 30, 90 mg/kg
Administration:P.o.; twice daily orally for 14 days
Result:Dose-dependently reduced tumor growth.
体外研究：
Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood.Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride 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：
Talmapimod hydrochloride (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:10, 30, 90 mg/kg
Administration:P.o.; twice daily orally for 14 days
Result:Dose-dependently reduced tumor growth.
体外研究：
Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood.Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
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