
Gemcitabine (elaidate)
CAS No. 210829-30-4
Gemcitabine (elaidate)( CP-4126 | CO-101 | Gemcitabine 5'-elaidate )
Catalog No. M23957 CAS No. 210829-30-4
Gemcitabine elaidate, is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity.?
Purity : >98% (HPLC)






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50MG | 388 | In Stock |
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Biological Information
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Product NameGemcitabine (elaidate)
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NoteResearch use only, not for human use.
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Brief DescriptionGemcitabine elaidate, is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity.?
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DescriptionGemcitabine elaidate, 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.
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In VitroGemcitabine elaidate (0.2 nM-1 mM; 72 h) inhibits the growth of gemcitabine sensitive and resistant cells, with IC50s of 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4 and MOLT4/C8 cells, respectively.Gemcitabine elaidate (0.5 nM-1 μM; 72 h) increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells. Cell Viability Assay Cell Line:A549 and WiDR cells Concentration:0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM Incubation Time:72 h Result:Induced a G2/M and S phase accumulation.
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In VivoGemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) inhibits the solid tumor xenografts growth of non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), pancreatic cancer (PANC-1).Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) shows acceptable toxicity and significant antitumor activity in the colon cancer xenograft Co6044 bearing mice.Gemcitabine elaidate (p.o. once daily for 5 doses) shows a favorable toxicity and antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044. Animal Model:Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively Dosage:25-120 mg/kg Administration:I.p. every 3 days for 5 doses Result:Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.
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SynonymsCP-4126 | CO-101 | Gemcitabine 5'-elaidate
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PathwayAutophagy
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TargetAutophagy
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RecptorAutophagy|Apoptosis
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Research Area——
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Indication——
Chemical Information
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CAS Number210829-30-4
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Formula Weight527.64
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Molecular FormulaC27H43F2N3O5
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Purity>98% (HPLC)
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SolubilityDMSO:26 mg/mL (49.28 mM);H2O:< 0.1 mg/mL (insoluble)
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SMILESCCCCCCCC/C=C/CCCCCCCC(OC[C@H]1O[C@@H](N2C=CC(N)=NC2=O)C(F)(F)[C@@H]1O)=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
molnova catalog



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