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LY2334737

LY2334737

  • CAT Number: I005340
  • CAS Number: 892128-60-8
  • Molecular Formula: C17H25F2N3O5
  • Molecular Weight: 389.39
  • Purity: ≥95%
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LY2334737 (Cat.No:I005340) is a selective inhibitor of Janus kinase 2 (JAK2). It is a small molecule drug that has been studied for its potential in the treatment of myeloproliferative neoplasms, including polycythemia vera and myelofibrosis. LY2334737 works by inhibiting the activity of JAK2, which plays a critical role in the signaling pathways involved in these diseases.

Catalog Number I005340
CAS Number 892128-60-8
Synonyms

N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]-2-propylpentanamide

Molecular Formula

C17H25F2N3O5

Purity 95%
Target Nucleoside Antimetabolite/Analogue
Solubility 10 mM in DMSO
Storage Store at -20℃
IUPAC Name N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]-2-propylpentanamide
InChI InChI=1S/C17H25F2N3O5/c1-3-5-10(6-4-2)14(25)20-12-7-8-22(16(26)21-12)15-17(18,19)13(24)11(9-23)27-15/h7-8,10-11,13,15,23-24H,3-6,9H2,1-2H3,(H,20,21,25,26)/t11-,13-,15-/m1/s1
InChIKey MEOYFIHNRBNEPI-UXIGCNINSA-N
SMILES CCCC(CCC)C(=O)NC1=NC(=O)N(C=C1)C2C(C(C(O2)CO)O)(F)F
Reference

</br>1:Phase I dose escalation and pharmacokinetic evaluation of two different schedules of LY2334737, an oral gemcitabine prodrug, in patients with advanced solid tumors. Faivre SJ, Olszanski AJ, Weigang-Köhler K, Riess H, Cohen RB, Wang X, Myrand SP, Wickremsinhe ER, Horn CL, Ouyang H, Callies S, Benhadji KA, Raymond E.Invest New Drugs. 2015 Dec;33(6):1206-16. doi: 10.1007/s10637-015-0286-7. Epub 2015 Sep 16. PMID: 26377590 </br>2:Phase 1b study of the oral gemcitabine /’Pro-drug/’ LY2334737 in combination with capecitabine in patients with advanced solid tumors. Infante JR, Benhadji KA, Dy GK, Fetterly G, Ma WW, Bendell J, Callies S, Adjei AA.Invest New Drugs. 2015 Apr;33(2):432-9. doi: 10.1007/s10637-015-0207-9. Epub 2015 Feb 3. PMID: 25640850 </br>3:Phase 1 dose escalation and pharmacokinetic evaluation of oral gemcitabine prodrug (LY2334737) in combination with docetaxel in patients with advanced solid tumors. Salazar R, Morales S, Gil-Martín M, Aguirre E, Oaknin A, Garcia M, Callies S, Wickremsinhe ER, Benhadji KA, Llombart A.Cancer Chemother Pharmacol. 2014 Jun;73(6):1205-15. doi: 10.1007/s00280-014-2457-1. Epub 2014 Apr 18. PMID: 24744161 </br>4:High sensitive assay employing column switching chromatography to enable simultaneous quantification of an amide prodrug of gemcitabine (LY2334737), gemcitabine, and its metabolite dFdU in human plasma by LC-MS/MS. Wickremsinhe ER, Lee LB, Schmalz CA, Torchia J, Ruterbories KJ.J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Aug 1;932:117-22. doi: 10.1016/j.jchromb.2013.06.008. Epub 2013 Jun 13. PMID: 23831704 </br>5:Phase I study of oral gemcitabine prodrug (LY2334737) in Japanese patients with advanced solid tumors. Yamamoto N, Nokihara H, Yamada Y, Uenaka K, Sekiguchi R, Makiuchi T, Slapak CA, Benhadji KA, Tamura T.Cancer Chemother Pharmacol. 2013 Jun;71(6):1645-55. doi: 10.1007/s00280-013-2165-2. Epub 2013 Apr 25. PMID: 23616084 </br>6:Efficacy of low-dose oral metronomic dosing of the prodrug of gemcitabine, LY2334737, in human tumor xenografts. Pratt SE, Durland-Busbice S, Shepard RL, Donoho GP, Starling JJ, Wickremsinhe ER, Perkins EJ, Dantzig AH.Mol Cancer Ther. 2013 Apr;12(4):481-90. doi: 10.1158/1535-7163.MCT-12-0654. Epub 2013 Jan 31. PMID: 23371859 Free Article</br>7:Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells. Pratt SE, Durland-Busbice S, Shepard RL, Heinz-Taheny K, Iversen PW, Dantzig AH.Clin Cancer Res. 2013 Mar 1;19(5):1159-68. doi: 10.1158/1078-0432.CCR-12-1184. Epub 2013 Jan 16. PMID: 23325581 Free Article</br>8:Low-dose metronomic oral dosing of a prodrug of gemcitabine (LY2334737) causes antitumor effects in the absence of inhibition of systemic vasculogenesis. Francia G, Shaked Y, Hashimoto K, Sun J, Yin M, Cesta C, Xu P, Man S, Hackl C, Stewart J, Uhlik M, Dantzig AH, Foster FS, Kerbel RS.Mol Cancer Ther. 2012 Mar;11(3):680-9. doi: 10.1158/1535-7163.MCT-11-0659. Epub 2011 Dec 21. PMID: 22188817 Free PMC Article</br>9:Phase I study of Oral gemcitabine prodrug (LY2334737) alone and in combination with erlotinib in patients with advanced solid tumors. Koolen SL, Witteveen PO, Jansen RS, Langenberg MH, Kronemeijer RH, Nol A, Garcia-Ribas I, Callies S, Benhadji KA, Slapak CA, Beijnen JH, Voest EE, Schellens JH.Clin Cancer Res. 2011 Sep 15;17(18):6071-82. doi: 10.1158/1078-0432.CCR-11-0353. Epub 2011 Jul 13. PMID: 21753156 Free Article

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