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Submit ReviewNSC 663284 is a potent, selective inhibitor of Cdc25 dual specificity phosphatases (Ki values are 29, 95 and 89 nM for human Cdc25A, Cdc25B2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. Arrests cells at both G1 and G2/M phase and blocks cdk2 and cdk1 activation. Blocks proliferation of a range of human tumor cell lines (IC50 = 0.2 - 35 μM).
NSC 663284 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 321.76 |
公式 | C15H16ClN3O3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 383907-43-5 |
PubChem ID | 379077 |
InChI Key | BMKPVDQDJQWBPD-UHFFFAOYSA-N |
Smiles | ClC1=C(NCCN2CCOCC2)C(=O)C2=NC=CC=C2C1=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 16.1 | 50 | |
ethanol | 16.1 | 50 |
以下数据基于产品分子量 321.76。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 6.22 mL | 31.08 mL | 62.16 mL |
2.5 mM | 1.24 mL | 6.22 mL | 12.43 mL |
5 mM | 0.62 mL | 3.11 mL | 6.22 mL |
25 mM | 0.12 mL | 0.62 mL | 1.24 mL |
参考文献是支持产品生物活性的出版物。
Brisson et al (2005) Redox regulation of cdc25B by cell-active Quinolinediones. Mol.Pharmacol. 68 1810 PMID: 16155209
Lazo et al (2001) Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J.Med.Chem. 44 4042 PMID: 11708908
Pu et al (2002) Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 7-chloro-6-(2-morpholin-4-ylethylamino)-quinoline-5,8-dione. J.Biol.Chem. 277 46877 PMID: 12356752
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