中文名 | 他匹莫德 |
英文名 | Talmapimod |
别名 | 他匹莫德 P38抑制剂(SCIO-469) 6-氯-5-[[(2R,5S)-4-[(4-氟苯基)甲基]-2,5-二甲基-1-哌嗪基]甲酰基]-N,N,1-三甲基-ALPHA-氧代-1H-吲哚-3-乙酰胺 6-氯-5-[[(2R,5S)-4-[(4-氟苯基)甲基]-2,5-二甲基-1-哌嗪基]甲酰基]-N,N,1-三甲基-alpha-氧代-1H-吲哚-3-乙酰胺 |
英文别名 | SCIO469 SCIO 469 TALMAPIMOD Talmapimod talmapimod Unii-B1E00kq6nt SCIO 469 - Talmapimod SCIO 469 hydrochloride 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)Methyl]-2,5-diMethyl-1-piperazinyl]carbonyl]-N,N,1-triMethyl-α-oxo-1H-indole-3-acetaMide 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-alpha-oxo-1H-indole-3-acetamide 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamidehydrochloride |
CAS | 309913-83-5 |
化学式 | C27H30ClFN4O3 |
分子量 | 513 |
密度 | 1.29 |
沸点 | 658.0±65.0 °C(Predicted) |
酸度系数 | 6.52±0.70(Predicted) |
存储条件 | Desiccate at +4°C |
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. Western Blot Analysis Cell Line: MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines Concentration: 100, 200 nM Incubation Time: 1 hour Result: Strongly inhibits phosphorylation of p38 MAPK. |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.949 ml | 9.747 ml | 19.493 ml |
5 mM | 0.39 ml | 1.949 ml | 3.899 ml |
10 mM | 0.195 ml | 0.975 ml | 1.949 ml |
5 mM | 0.039 ml | 0.195 ml | 0.39 ml |
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