他匹莫德

生物活性靶点体外研究体内研究他匹莫德试剂级价格

他匹莫德

CAS号:309913-83-5
英文名:talmapimod
中文名:他匹莫德
CBNumber:CB81518535
分子式:C27H30ClFN4O3
分子量:513
MOL File:309913-83-5.mol

他匹莫德化学性质

沸点 :658.0±65.0 °C(Predicted)
密度 :1.29
储存条件 :Desiccate at +4°C
溶解度 :DMSO: soluble
形态 :A crystalline solid
酸度系数(pKa) :6.52±0.70(Predicted)
颜色 :Pink to red

安全信息

海关编码 :2924297099

他匹莫德性质、用途与生产工艺

生物活性 Talmapimod (他匹莫德; SCIO-469) 是 p38α 选择性的，具有口服活性的，ATP 竞争性的抑制剂，IC50 值是 9 nM，约为 p38β 的10倍，在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。
靶点

p38α

9 nM (IC ₅₀ )

p38β

90 nM (IC ₅₀ )

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.