DA-3003-1

SKU: orb1706897

Description

DA-3003-1 is a cell-permeable, potent, and selective inhibitor of Cdc25 dual-specificity phosphatases (A, B, and C isoforms). Its ability to disrupt cell cycle progression has demonstrated antitumor activity, making it a valuable chemical probe for studying cell cycle regulation and oncology in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Metabolism Research

Key Properties

• CAS Number: 383907-43-5
• MW: 321.76
• Purity: 99.79% (May vary between batches)
• Formula: C₁₅H₁₆ClN₃O₃
• SMILES: ClC1=C(NCCN2CCOCC2)C(=O)c2ncccc2C1=O
• Target: Histone Methyltransferase,Phosphatase
• Solubility: DMSO:60 mg/mL (186.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.22 mM)

Bioactivity

• Target IC50:
  MCF-7 cells:1.7 μM|MDA-MB-435 cells:0.2 μM|NCI-60 cells:1.5±0.6 μM|CDC25B2:0.21 μM
• 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.
• 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. 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).

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDC25A, Cdc25B2, CDC25B2, CDC25C, NSC 663284

Compound Identifiers

PubChem CID

379077