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NSC 663284

Cayman Chemical Item Number 13303

Cdc25 Phosphatase Inhibitor II; DA-3003-1 (CAS 383907-43-5)

NSC 663284 (CAS 383907-43-5)

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Description

Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).1 NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).1,2 By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,3,4 arrests cells at both G1 and G2/M phases,3 and prevents the proliferation of several human tumor cell lines.1,3,5

1 Lazo, J.S., Aslan, D.C., Southwick, E.C., et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem 44 4042-4049 (2001).

2 Vogt, A., McDonald, P.R., Tamewitz, A., et al. A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. Mol Cancer Ther 7(2) 330-340 (2008).

3 Pu, L., Amoscato, A.A., Bier, M.E., et al. 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(49) 46877-46885 (2002).

4 Han, Y., Shen, H., Carr, B.I., et al. NAD(P)H:quinone oxidoreductase-1-dependent and -independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors. J Pharmacol Exp Ther 309(1) 64-70 (2004).

5 Guo, J., Parise, R.A., Joseph, E., et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res 27 3067-3074 (2007).

Synonyms
  • Cdc25 Phosphatase Inhibitor II
  • DA-3003-1
Formal Name 6-​chloro-​7-​[[2-​(4-​morpholinyl)ethyl]amino]-​5,​8-​quinolinedione
CAS Number 383907-43-5
Molecular Formula C15H16ClN3O3
Formula Weight 321.8
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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ClC1=C(NCCN2CCOCC2)​C(=O)​c2ncccc2C1=O

Background Reading

Pu, L., Amoscato, A.A., Bier, M.E., et al. 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(49) 46877-46885 (2002).

Guo, J., Parise, R.A., Joseph, E., et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res 27 3067-3074 (2007).

Vogt, A., McDonald, P.R., Tamewitz, A., et al. A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. Mol Cancer Ther 7(2) 330-340 (2008).

Han, Y., Shen, H., Carr, B.I., et al. NAD(P)H:quinone oxidoreductase-1-dependent and -independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors. J Pharmacol Exp Ther 309(1) 64-70 (2004).

Lazo, J.S., Aslan, D.C., Southwick, E.C., et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem 44 4042-4049 (2001).

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Size Price Quantity Subtotal
1 mg $21.00 $0.00
5 mg $95.00 $0.00
10 mg $168.00 $0.00
25 mg $368.00 $0.00
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Pricing updated 2012-05-26. Prices are subject to change without notice.

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