化合物TAK-441 T21325

Product Introduction
Bioactivity


英文名: TAK-441

描述: TAK-441 是一种具有口服活性的 Hedgehog 信号抑制剂 (IC50 = 4.4 nM)，具有有效的抗肿瘤活性。 TAK-441 抑制转录因子 Gli1 mRNA 表达和肿瘤生长。

体外活性: TAK-441 (0.03 nM–1 μM) inhibits Gli1 mRNA in the tumor and skin with IC50s of 45.7 and 113 μg/ml, respectively[3]. In LNCaP cells, TAK-441 (0.5-500 nM) delays the castration-resistant progression without affecting androgen withdrawal-induced Shh up-regulation or cell viability[4].

体内活性: In ptc1+/-p53-/- mice, oral administration of TAK-441 (1-25 mg/kg) shows strong and dose-dependent antitumor activity. In BALB/c-nu/nu mice, oral administration of TAK-441 (10-100 mg/kg) shows favorable exposure and good oral absorption[4].

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

溶解度: DMSO : 45 mg/mL (78.05 mM)
H2O : Insoluble


关键字: TAK 441 | TAK-441

相关产品: SAG 21k | Sonidegib | Naftifine hydrochloride | Taladegib | SAG hydrochloride (912545-86-9(free base)) | Hh-Ag1.5 | GANT 61 | SMO-IN-2 | Ciliobrevin D | MK-4101

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Stem Cell Differentiation 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