他匹莫德 T12871

Product Introduction
Bioactivity


英文名: Talmapimod

描述: 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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 95 mg/mL (185.19 mM)


关键字: cytotoxicity | multiple | inhibit | tumor | SCIO469 | cells | Hsp27 | Inhibitor | phosphorylation | p38 MAPK | Talmapimod | SCIO 469 | myeloma

相关产品: Isofraxidin | Sauchinone | Dihydrocaffeic acid | Esculin | Lucidenic acid F | PF-3644022 | Cristacarpin | Selinidin | Isochamaejasmine | PLK1/p38γ-IN-1

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途