CP-724714

SKU: orb1223133

Description

CP-724714 is An orally bioavailable quinazoline with potential antineoplastic activity. CP-724,714 selectively binds to the intracellular domain of HER2, reversibly inhibiting its tyrosine kinase activity and resulting in suppression of tumor cell growth. HER2, a member of the epidermal growth factor receptor (EGFR) family, is overexpressed in many adenocarcinomas, particularly breast cancers.

Key Properties

• CAS Number: 383432-38-0
• MW: 469.54
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₇N₅O₃
• SMILES: Cc1ncc(cc1)Oc1c(cc(cc1)Nc1ncnc2c1cc(cc2)/C=C/CNC(=O)COC)C
• Target: Cannabinoid Receptor
• Solubility: DMSO : ≥ 50 mg/mL; 106.49 mM

Bioactivity

• In Vivo:
  CP-724714 (3.25-100 mg/kg; p.o. ; 0.5-8 hours) results in a concentration-dependent reduction of ErbB2 receptor phosphorylation. CP-724714 (6.25-100 mg/kg; p.o. ; q. d; for 8 to 40 day) inhibits FRE-erbB2 xenograft growth. CP-724714 (Athymic, female FRE-erbB2 xenograft-bearing mice; 30 or 100 mg/kg; p.o.) treatments results in a time-and dose-dependent induction of apoptosis, which was evident as early as 4 to 8 h after dosing. Approximately 75% more tumor cells exhibited apoptotic changes in the 100 mg/kg treatment group compared with vehicle control group at 8 h after dosing. CP-724714 induces regression of BT-474 tumors and significant inhibition in a number of other human tumor xenografts. Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue. Animal model: Female athymic mice (bearing FRE-erbB2 xenografts). Dosage: 3.25-100 mg/kg. Administration: p.o. ; 0.5-8 hours. Result: Produced a reduction of erbB2 tyrosine phosphorylation in FRE-erbB2 xenografts. Animal model: Athymic female mice bearing FRE-erbB2 xenografts. Dosage: 6.25-100 mg/kg. Administration: p.o. ; q. d; for 8 to 40 day. Result: Resulted in an inhibition of FRE-erbB2 xenografts.
• In Vitro:
  CP-724714 is >1, 000-fold less potent for insulin receptor, insulin-like growth factor-I receptor, platelet-derived growth factor β, vascular endothelial growth factor 2, Abl, Src, c-Met, JNK-2, JNK-3, ZAP-70, Cdk-2, and Cdk-5.CP-724714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain at a concentration as low as 50 nmol/L (IC50 = 32 nM) but is markedly less potent against EGFR. CP-724714 (1 μM; 24 hours) induces G1 cell cycle block in vitro in erbB2-overexpressing BT-474 human breast carcinoma cells. Cell Cycle Analysis Cell line: erbB2-amplified BT-474 breast cancer cells. Concentration: 1 μM. Incubation time: 24 hours. Result: Resulted in accumulation of cells in G1 phase and a marked reduction in S-phase cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP724714 | CP 724714 | CP-724714

Quick Database Links

Gene Symbol

Cannabinoid Receptor