NSC 663284

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Cat.No. 1867 - NSC 663284 | C15H16ClN3O3 | CAS No. 383907-43-5
Description: Potent, selective Cdc25 phosphatase inhibitor
Chemical Name: 6-Chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione
Purity: ≥99% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

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).

Compound Libraries

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Technical Data

M. Wt 321.76
Formula C15H16ClN3O3
Storage Store at +4°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 16.1 50
ethanol 16.1 50

Preparing Stock Solutions

The following data is based on the product molecular weight 321.76. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.11 mL 15.54 mL 31.08 mL
5 mM 0.62 mL 3.11 mL 6.22 mL
10 mM 0.31 mL 1.55 mL 3.11 mL
50 mM 0.06 mL 0.31 mL 0.62 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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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