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.

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].

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].