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DA-3003-1 (DA-3003-1) 是一种可渗透进细胞膜且具有有效性和选择性的 Cdc25 dual specificity phosphatase 抑制剂,具有抗肿瘤活性,对 Cdc25B2、Cdc25A、Cdc25B2 和 Cdc25C具有抑制作用。
DA-3003-1 (DA-3003-1) 是一种可渗透进细胞膜且具有有效性和选择性的 Cdc25 dual specificity phosphatase 抑制剂,具有抗肿瘤活性,对 Cdc25B2、Cdc25A、Cdc25B2 和 Cdc25C具有抑制作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 259 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 818 | 现货 |
产品描述 | DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C. |
靶点活性 | CDC25B2:0.21 μM, NCI 60 cells:1.5±0.6 μM, MDA-MB-435:0.2 μM, MCF-7 cells:1.7 μM |
体外活性 | DA-3003-1(DA-3003-1)(3-100 μM; 48 hours) exhibits an average IC50 value of 1.5 ± 0.6 μM across the NCI 60 cell panel of human tumor types. The IC50 values for human breast cancer MDA-MB-435 and MDA-N cells are 0.2 μM, while in cultured human breast MCF-7 cells, the IC50 value is 1.7 μM[1]. The relative IC50 value of DA-3003-1(DA-3003-1) against Cdc25B2 (IC50=0.21 μM) is lower than that against VHR (IC50 20 times lower and 450 times lower than 4.0 μM) or PTP1B (IC50>4.0 μM)[3]. |
体内活性 | DA-3003-1(DA-3003-1)(intravenous injection; 2, 3, and 5 mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. Following a single dose of 5 mg/kg, DA-3003-1(DA-3003-1)is undetectable in plasma or tissues for more than 5 minutes. After treatment of HT29 tumor-bearing SCID mice with DA-3003-1(DA-3003-1), a greater reduction in glutathione concentration is observed in the tumor compared to the liver and kidneys, and this decrease persists for a longer duration[1]. |
别名 | NSC 663284 |
分子量 | 321.76 |
分子式 | C15H16ClN3O3 |
CAS No. | 383907-43-5 |
存储 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (186.47 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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