NSC 663284 is a cell-permeable and irreversible Cdc25 dual specificity phosphatase inhibitor (IC50 for Cdc25B2: 0.21 μM). NSC 663284 inhibits NSD2 (IC50 of 170 nM) through direct interaction with the catalytic SET domain (Kd of 370 nM). NSC 663284 displays mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively.

NSC 663284 has relative IC50 values for Cdc25B2 (IC50=0.21 μM) are 20- and 450-fold lower than for VHR (IC50=4.0 μM) or PTP1B (IC50>4.0 μM), respectively. NSC 663284 (3-100μM; 48 hours) has a mean IC50 value in the NCI 60 Cell human tumor panel of 1.5 ± 0.6 μM. NSC 663284 (3-100μM; 48 hours) has IC50 values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells. NSC 663284 (3-100μM; 48 hours) has an IC50 value of 1.7 μM in human breast MCF-7 cells in culture[1].

NSC 663284 is not detectable in plasma or tissues beyond 5 min, after a single dose of 5 mg/kg. NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. Following NSC 663284 treatment of tumor-bearing SCID mice, decreases glutathione concentrations in HT29 tumors are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in the liver and kidneys[3].

383907-43-5

C15H16ClN3O3

321.76

DA-3003-1;NSC 663284

DMSO:150 mg/mL (466.19 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years