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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 787 | 现货 | |
5 mg | ¥ 1,990 | 现货 | |
10 mg | ¥ 2,980 | 现货 | |
25 mg | ¥ 5,370 | 现货 | |
50 mg | ¥ 7,330 | 现货 | |
100 mg | ¥ 9,880 | 现货 |
产品描述 | TAK-441 is an orally active inhibitor of Hedgehog signaling(IC50 = 4.4 nM) with potent antitumor activity. TAK-441 suppresses transcription factor Gli1 mRNA expression and tumor growth. |
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]. |
别名 | TAK441 |
分子量 | 576.56 |
分子式 | C28H31F3N4O6 |
CAS No. | 1186231-83-3 |
Smiles | O(CC(F)(F)F)C=1C2=C(N(C)C1C(NC3CCN(C(CO)=O)CC3)=O)C=C(CC)N(CC(=O)C4=CC=CC=C4)C2=O |
密度 | 1.40 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 45 mg/mL (78.05 mM) H2O: Insoluble | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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