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
- 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
- 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 )
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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.
- 更新日期：2024/11/08
- 产品编号：HY-10406
- 产品名称：Talmapimod
- CAS编号：
- 包装：1 mg
- 价格：623元
- 更新日期：2024/11/08
- 产品编号：HY-10406
- 产品名称：他匹莫德 Talmapimod
- CAS编号：309913-83-5
- 包装：2mg
- 价格：900元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
