NSC 663284

NSC 663284化学性质

沸点 :478.8±45.0 °C(Predicted)
密度 :1.41±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: 16 mg/mL
形态 :solid
酸度系数(pKa) :6.79±0.10(Predicted)
颜色 :red
敏感性 :Light Sensitive
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

安全信息

NSC 663284性质、用途与生产工艺

生物活性 NSC 663284 是一种有效的，细胞可渗透的且不可逆的 Cdc25 dual specificity phosphatase 抑制剂，Cdc25B2 的 IC50 为 0.21 μM。NSC 663284 表现出与 Cdc25A，Cdc25B2 和 Cdc25C 的混合竞争动力学，Ki 值分别为 29、95 和 89 nM。NSC 663284 通过与 SET 结构域 (Kd of 370 nM) 的相互作用来抑制 NSD2 (IC50 of 170 nM) 酶的活性。
靶点

IC50: 0.21 μM (Cdc25B2)
体外研究

NSC 663284 (3-100μM; 48 hours) has a mean IC ₅₀ value in the NCI 60 Cell human tumor panel of 1.5 ± 0.6 μM, has IC ₅₀ values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells, has an IC ₅₀ value of 1.7 μM in human breast MCF-7 cells in culture. NSC 663284 has relative IC ₅₀ values for Cdc25B2 (IC ₅₀ =0.21 μM) are 20- and 450-fold lower than for VHR (IC ₅₀ =4.0 μM) or PTP1B (IC ₅₀ >4.0 μM), respectively.
体内研究

NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys.

NSC 663284上下游产品信息

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下游产品

NSC 663284生产厂家

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