TalmaPimod 是选择性的，可口服的，ATP 竞争性的p38α抑制剂，IC50值是 9 nM。

Talmapimod is a selective, orally active and ATP-competitive inhibitor of p38α(IC50 : 9 nM) .

phosphorylation of p38 MAPK inhibited by Talmapimod (100-200 nM; 1 hour) in MM cells[1].In human whole blood, LPS-induced TNF-a production inhibited by Talmapimod [2]. Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3].

Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden,and preventing the development of myeloma bone disease[2]. In 5T2MM and 5T33MM models，Talmapimod inhibits the growth of multiple myeloma and prevents bone diseases[3]. 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[4].

309913-83-5

C27H30ClFN4O3

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他匹莫德;SCIO-469

DMSO:95 mg/mL (185.19 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years