309913-83-5
309913-83-5 結(jié)構(gòu)式
基本信息
P38抑制劑(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
Scios 469
talmapimod
Unii-B1E00kq6nt
TalMapiMod (SCIO-469)
SCIO 469 - Talmapimod
SCIO 469 hydrochloride
Talmapimod hydrochloride
TALMAPIMOD
SCIO469
SCIO 469
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
物理化學(xué)性質(zhì)
常見問題列表
|
p38α 9 nM (IC 50 ) |
p38β 90 nM (IC 50 ) |
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. |
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. |