MedKoo Biosciences/CP-724714/200820/5mg

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.

MedKoo Cat#: 200820 Name: CP-724714 CAS#: 383432-38-0 Chemical Formula: C27H27N5O3 Exact Mass: 469.21139 Molecular Weight: 469.53 Elemental Analysis: C, 69.07; H, 5.80; N, 14.92; O, 10.22

Synonym: CP724714; CP 724714; CP-724714.

IUPAC/Chemical Name: (E)-2-methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)acetamide.

InChi Key: LLVZBTWPGQVVLW-SNAWJCMRSA-N

InChi Code: InChI=1S/C27H27N5O3/c1-18-13-21(8-11-25(18)35-22-9-6-19(2)29-15-22)32-27-23-14-20(7-10-24(23)30-17-31-27)5-4-12-28-26(33)16-34-3/h4-11,13-15,17H,12,16H2,1-3H3,(H,28,33)(H,30,31,32)/b5-4+

SMILES Code: O=C(NC/C=C/C1=CC2=C(NC3=CC=C(OC4=CC=C(C)N=C4)C(C)=C3)N=CN=C2C=C1)COC

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

                 

References

1: Feng B, Xu JJ, Bi YA, Mireles R, Davidson R, Duignan DB, Campbell S, Kostrubsky VE, Dunn MC, Smith AR, Wang HF. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol Sci. 2009 Apr;108(2):492-500. doi: 10.1093/toxsci/kfp033. Epub 2009 Feb 17. PubMed PMID: 19223659.

2: Jani JP, Finn RS, Campbell M, Coleman KG, Connell RD, Currier N, Emerson EO, Floyd E, Harriman S, Kath JC, Morris J, Moyer JD, Pustilnik LR, Rafidi K, Ralston S, Rossi AM, Steyn SJ, Wagner L, Winter SM, Bhattacharya SK. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res. 2007 Oct 15;67(20):9887-93. PubMed PMID: 17942920.

3: Guo F, Letrent SP, Munster PN, Britten CD, Gelmon K, Tolcher AW, Sharma A. Pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors: correlations with clinical characteristics and safety. Cancer Chemother Pharmacol. 2008 Jun;62(1):97-109. Epub 2007 Sep 6. PubMed PMID: 17805538.

4: Munster PN, Britten CD, Mita M, Gelmon K, Minton SE, Moulder S, Slamon DJ, Guo F, Letrent SP, Denis L, Tolcher AW. First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors. Clin Cancer Res. 2007 Feb 15;13(4):1238-45. PubMed PMID: 17317835.

5: Guo F, Letrent SP, Sharma A. Population pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors. Cancer Chemother Pharmacol. 2007 Nov;60(6):799-809. Epub 2007 Feb 7. PubMed PMID: 17285315.