Your shopping cart is empty!
Anba Pharma Gemcitabine elaidate CAS No.: 210829-30-4 .. Product #: Anba-000965 Regular price: $140.00 $140.00

Gemcitabine elaidate

Catalog No.: Anba-000965
Weight: 10mg

Price: $140.00

Available Options

* Weight:
- +

Gemcitabine elaidate, also known as CO-101 and CP-4126, is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.

1: Poplin E, Wasan H, Rolfe L, Raponi M, Ikdahl T, Bondarenko I, Davidenko I, Bondar V, Garin A, Boeck S, Ormanns S, Heinemann V, Bassi C, Evans TR, Andersson R, Hahn H, Picozzi V, Dicker A, Mann E, Voong C, Kaur P, Isaacson J, Allen A. Randomized, Multicenter, Phase II Study of CO-101 Versus Gemcitabine in Patients With Metastatic Pancreatic Ductal Adenocarcinoma: Including a Prospective Evaluation of the Role of hENT1 in Gemcitabine or CO-101 Sensitivity. J Clin Oncol. 2013 Dec 10;31(35):4453-61. doi: 10.1200/JCO.2013.51.0826. Epub 2013 Nov 12. PubMed PMID: 24220555.
2: Stuurman FE, Lolkema MP, Huitema AD, Soetekouw PM, Rosing H, Rolfe L, Kaur P, Beijnen JH, van Tinteren H, Voest EE, Schellens JH. A phase 1 comparative pharmacokinetic and cardiac safety study of two intravenous formulations of CO-101 in patients with advanced solid tumors. J Clin Pharmacol. 2013 Aug;53(8):878-83. doi: 10.1002/jcph.108. Epub 2013 Jun 18. PubMed PMID: 23775853.
3: Stuurman FE, Voest EE, Awada A, Witteveen PO, Bergeland T, Hals PA, Rasch W, Schellens JH, Hendlisz A. Phase I study of oral CP-4126, a gemcitabine derivative, in patients with advanced solid tumors. Invest New Drugs. 2013 Aug;31(4):959-66. doi: 10.1007/s10637-013-9925-z. Epub 2013 Jan 24. PubMed PMID: 23345000.
4: Adema AD, Smid K, Losekoot N, Honeywell RJ, Verheul HM, Myhren F, Sandvold ML, Peters GJ. Metabolism and accumulation of the lipophilic deoxynucleoside analogs elacytarabine and CP-4126. Invest New Drugs. 2012 Oct;30(5):1908-16. doi: 10.1007/s10637-011-9756-8. Epub 2011 Oct 15. PubMed PMID: 22002019; PubMed Central PMCID: PMC3432794.
5: Sandvold ML, Galmarini C, Myhren F, Peters G. The activity of the lipophilic nucleoside derivatives elacytarabine and CP-4126 in a panel of tumor cell lines resistant to nucleoside analogues. Nucleosides Nucleotides Nucleic Acids. 2010 Jun;29(4-6):386-93. doi: 10.1080/15257771003729625. PubMed PMID: 20544524.
6: Bergman AM, Adema AD, Balzarini J, Bruheim S, Fichtner I, Noordhuis P, Fodstad O, Myhren F, Sandvold ML, Hendriks HR, Peters GJ. Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models. Invest New Drugs. 2011 Jun;29(3):456-66. doi: 10.1007/s10637-009-9377-7. Epub 2010 Jan 12. PubMed PMID: 20066470; PubMed Central PMCID: PMC3076580.
7: Adema AD, Laan AC, Myhren F, Fichtner I, Verheul HM, Sandvold ML, Peters GJ. Cell cycle effects of fatty acid derivatives of cytarabine, CP-4055, and of gemcitabine, CP-4126, as basis for the interaction with oxaliplatin and docetaxel. Int J Oncol. 2010 Jan;36(1):285-94. PubMed PMID: 19956857.
8: Galmarini CM, Myhren F, Sandvold ML. CP-4055 and CP-4126 are active in ara-C and gemcitabine-resistant lymphoma cell lines. Br J Haematol. 2009 Jan;144(2):273-5. doi: 10.1111/j.1365-2141.2008.07467.x. Epub 2008 Nov 19. PubMed PMID: 19036103.
Chemical
CAS Num 210829-30-4
Chemical Formula C27H43F2N3O5
Molecular Weight 527.644
IUPAC Chemical Name (E)-((2R,3R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-4,4-difluoro-3-hydroxytetrahydrofuran-2-yl)methyl octadec-9-enoate.
Exact Mass 527.31708
Elemental Analysis C, 61.46; H, 8.21; F, 7.20; N, 7.96; O, 15.16
Synonym CO101; CO-101; CO 101; CP4126; CP-4126; CP 4126; Gemcitabine elaidate.
Solubility Soluble in DMSO, not in water
SMILES Code CCCCCCCC/C=C/CCCCCCCC(OC[C@H]1O[C@@H](N2C=CC(N)=NC2=O)C(F)(F)[C@@H]1O)=O
Biological
Targets and Effects ribonucleotide reductase inhibitor
Pathways Apoptosis
Physical
Appearance white 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).
Shelf Life >2 years if stored properly

Mailing Address

Anba Pharma Company
3-H Gill Street, Suite 300
Woburn, MA 01801
United State

Our Contact Info.

Tel: 1+610-883-0668

Email: sales@AnbaPharma.com

Subscribe to our Newsletter

Stay Updated With Our Latest Products.

Please publish modules in offcanvas position.