CP-724714

Research use only, not for human use.

CP-724714 is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.

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.

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.

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 xenograftsDosage:6.25- 100 mg/kg Administration:P.o.; q.d; for 8 to 40 day Result:Resulted in an inhibition of FRE-erbB2 xenografts.

CP724714 | CP 724714 | CP-724714

GPCR/G Protein

Cannabinoid Receptor

HER2/ErbB2

Cancer

——

383432-38-0

469.54

C27H27N5O3

>98% (HPLC)

DMSO : ≥ 50 mg/mL; 106.49 mM

Cc1ncc(cc1)Oc1c(cc(cc1)Nc1ncnc2c1cc(cc2)/C=C/CNC(=O)COC)C

(E)-2-methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)acetamide.

(-20℃)

With Ice Pack

≥ 2 years