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ChemicalBook Product Catalog CP 461

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CP 461 NEW

$195.00 1mg

$430.00 5mg

$636.00 10mg

Min. Order
Purity99.57%
Cas No227619-96-7
Supply Ability10g
Update time2024-11-19

TargetMol Chemicals Inc.

TargetMol Chemicals Inc.

5YR

United States

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Chemical Properties

Product Name	CP 461
CAS No	227619-96-7
EC-No
Min. Order
Purity	99.57%
Supply Ability	10g
Release date	2024/11/19

Product Introduction

Bioactivity

Name	CP 461
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]
Storage	Powder: -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)
Keywords	OSI-461 \| OSI461 \| CP 461
Inhibitors Related	Stavudine \| 5-Fluorouracil \| Acetylcysteine \| Kaempferol \| Myricetin \| Sodium 4-phenylbutyrate \| L-Ascorbic acid \| Dextran sulfate sodium salt (MW 4500-5500) \| Metronidazole \| Sorafenib \| Tributyrin \| Lidocaine hydrochloride
Related Compound Libraries	Bioactive Compound Library \| Anti-Cancer Clinical Compound Library \| Drug Repurposing Compound Library \| Inhibitor Library \| Clinical Compound Library \| Bioactive Compounds Library Max \| Anti-Cancer Compound Library \| Anti-Cancer Active Compound Library \| Anti-Cancer Drug Library

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