NSC 663284
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- CAS号:
- 383907-43-5
- 英文名:
- NSC 663284
- 英文别名:
- NSC 663284 (DA3003-1);CDC25 Phosphatase Inhibitor II, NSC 663284;5,8-Quinolinedione, 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-;CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem
- 中文名:
- NSC 663284
- 中文别名:
- 化合物 T16357;NSC 663284(DA3003-1),CDC25抑制剂
- CBNumber:
- CB1504040
- 分子式:
- C15H16ClN3O3
- 分子量:
- 321.76
- MOL File:
- 383907-43-5.mol
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NSC 663284化学性质
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沸点:
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478.8±45.0 °C(Predicted)
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密度:
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1.41±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 16 mg/mL
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形态:
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solid
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酸度系数(pKa):
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6.79±0.10(Predicted)
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颜色:
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red
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敏感性:
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Light Sensitive
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稳定性:
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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.
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NSC 663284性质、用途与生产工艺
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。
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
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values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells, has an IC
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value of 1.7 μM in human breast MCF-7 cells in culture.
NSC 663284 has relative IC
50
values for Cdc25B2 (IC
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=0.21 μM) are 20- and 450-fold lower than for VHR (IC
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=4.0 μM) or PTP1B (IC
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>4.0 μM), respectively.
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
上游原料
下游产品
383907-43-5, NSC 663284 相关搜索:
- Protein Phosphatase
- 药靶配体
- NSC 663284(DA3003-1),CDC25抑制剂
- 化合物 T16357
- 383907-43-5
- NSC 663284 (DA3003-1)
- CDC25 Phosphatase Inhibitor II, NSC 663284
- 5,8-Quinolinedione, 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-
- CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem