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DA-3003-1

Catalog No. T16357   CAS 383907-43-5
Synonyms: NSC 663284

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

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DA-3003-1 Chemical Structure
DA-3003-1, CAS 383907-43-5
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1 mL * 10 mM (in DMSO) In stock $ 30.00
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Purity: 99.79%
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Biological Description
Chemical Properties
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Description DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.
Targets&IC50 NCI 60 cell:1.5±0.6 μM, MDA-MB-435:0.2 μM, MCF-7 cells:1.7 μM, Cdc25B2:0.21 μM
In vitro DA-3003-1(DA-3003-1)(3-100 μM; 48 hours) exhibits an average IC50 value of 1.5 ± 0.6 μM across the NCI 60 cell panel of human tumor types. The IC50 values for human breast cancer MDA-MB-435 and MDA-N cells are 0.2 μM, while in cultured human breast MCF-7 cells, the IC50 value is 1.7 μM[1].
The relative IC50 value of DA-3003-1(DA-3003-1) against Cdc25B2 (IC50=0.21 μM) is lower than that against VHR (IC50 20 times lower and 450 times lower than 4.0 μM) or PTP1B (IC50>4.0 μM)[3].
In vivo DA-3003-1(DA-3003-1)(intravenous injection; 2, 3, and 5 mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. Following a single dose of 5 mg/kg, DA-3003-1(DA-3003-1)is undetectable in plasma or tissues for more than 5 minutes. After treatment of HT29 tumor-bearing SCID mice with DA-3003-1(DA-3003-1), a greater reduction in glutathione concentration is observed in the tumor compared to the liver and kidneys, and this decrease persists for a longer duration[1].
Synonyms NSC 663284
Molecular Weight 321.76
Formula C15H16ClN3O3
CAS No. 383907-43-5

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL(186.47 mM)

TargetMolReferences and Literature

1. Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res. 2007 Sep-Oct;27(5A):3067-73. 2. Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSDJ Biol Chem. 2018 Aug 31;293(35):13750-13765. 3. Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9.

Related compound libraries

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Keywords

DA-3003-1 383907-43-5 Metabolism Phosphatase NSC 663284 inhibitor inhibit

 

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