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Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。

Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 455 | In stock | |
| 5 mg | ¥ 826 | In stock | |
| 10 mg | ¥ 1,530 | In stock | |
| 25 mg | ¥ 3,220 | In stock | |
| 50 mg | ¥ 4,670 | In stock | |
| 100 mg | ¥ 6,530 | In stock | |
| 200 mg | ¥ 8,780 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 932 | In stock |
Talmapimod 相关产品
| 产品描述 | Talmapimod (SCIO-469) is an selective, orally active, and ATP-competitive p38α inhibitor with IC50 of 9 nM and 90 nM for p38α and p38β, respectively. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs. |
| 靶点活性 | p38α:9 nM, p38β:90 nM |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 别名 | 他匹莫德, SCIO-469 |
| 分子量 | 513 |
| 分子式 | C27H30ClFN4O3 |
| CAS No. | 309913-83-5 |
| Smiles | C[C@H]1CN([C@H](C)CN1Cc1ccc(F)cc1)C(=O)c1cc2c(cn(C)c2cc1Cl)C(=O)C(=O)N(C)C |
| 密度 | 1.29 g/cm3 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 95 mg/mL (185.19 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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DMSO
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