CP 461

SKU: orb1697727

Description

CP 461 (UNII-68OJX9I7DT) is a selective PDE2A inhibitor that induces apoptosis in various human cancer cell lines in vitro while sparing normal cells. Its research applications include studying cyclic nucleotide signaling in oncology and exploring its potential in preclinical cancer models.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 227619-96-7
• MW: 420.91
• Purity: 99.82% (May vary between batches)
• Formula: C₂₅H₂₂ClFN₂O
• SMILES: C(C(NCC1=CC=CC=C1)=O)C=2C=3C(/C(=C\C=4C=CN=CC4)/C2C)=CC=C(F)C3.Cl
• Target: PDE,Microtubule Associated,Apoptosis
• Solubility: DMSO:16.67 mg/mL (39.6 mM)

Bioactivity

• In Vivo:
  CP-461 inhibits the growth of a broad range of human tumor cell lines in vitro at micromolar concentrations and selectively induces apoptosis in cancer cell lines but not normal cells. Preclinical studies revealed good oral bioavailability and no toxicity in dogs and rats at single doses of up to 500 mg/kg. In a Phase I trial, 21 patients with a range of solid tumors and good performance status received CP-461 p.o. twice daily for 28 consecutive days. Cycles were repeated without a treatment-free interval. CP-461 doses ranged from 100 to 800 mg/day. Therapy was well tolerated overall, and a maximum tolerated dose was not reached. Grade 3 asymptomatic aspartate aminotransferase/alanine aminotransferase elevation in 1 patient treated at 800 mg/day was the only dose-limiting toxicity. No hematologic toxicity was noted. Peak plasma concentrations occurred between 1 and 2 h after dosing, and doses above 200 mg/day exceeded the known in vitro EC(50) (1-2 micro M) for apoptosis in cancer cells. No drug was detectable after 24 h of administration, and the terminal half-life was 6.7 h. The area under the plasma concentration-time curve was dose-proportional from 200 to 800 mg/day. Four patients exhibited disease stability after two cycles of treatment. CP-461 is minimally toxic at doses up to 800 mg/day when administered p.o. on a twice-daily schedule.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, CP 461, CP461, CP-461, PDE2, UNII-68OJX9I7DT, OSI 461, OSI461, OSI-461

Compound Identifiers

PubChem CID

6445781