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CP 461

CP 461
CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.
Catalog No. T31020Cas No. 227619-96-7
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Purity:99.57%
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CP 461

Catalog No. T31020Alias UNII-68OJX9I7DT, OSI 461, CP-461, CP461Cas No. 227619-96-7

CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.
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Pack SizePriceAvailabilityQuantity
1 mg$195In Stock
5 mg$430In Stock
10 mg$636In Stock
25 mg$987In Stock
50 mg$1,360In Stock
100 mg$1,830In Stock
500 mg$3,680In Stock
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Product Introduction

Bioactivity
Description
CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.
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.[1]
AliasUNII-68OJX9I7DT, OSI 461, CP-461, CP461
Chemical Properties
Molecular Weight420.91
FormulaC25H22ClFN2O
Cas No.227619-96-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 16.67 mg/mL (39.6 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3758 mL11.8790 mL23.7580 mL118.7902 mL
5 mM0.4752 mL2.3758 mL4.7516 mL23.7580 mL
10 mM0.2376 mL1.1879 mL2.3758 mL11.8790 mL
20 mM0.1188 mL0.5940 mL1.1879 mL5.9395 mL

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