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Gemcitabine elaidate hydrochloride

Catalog No. T15378L CAS 2918768-08-6

Synonyms: CO-101 hydrochloride, Gemcitabine elaidate hydrochloride(210829-30-4(free base)), Gemcitabine 5'-elaidate hydrochloride, CP-4126 hydrochloride

Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. In contrast to gemcitabine, Gemcitabine elaidate hydrochloride could be administered orally, with a schedule and dose dependent toxicity and antitumor activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Gemcitabine elaidate hydrochloride Chemical Structure

Gemcitabine elaidate hydrochloride, CAS 2918768-08-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 185.00
50 mg	In stock	$ 337.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.6%

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Description	Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. In contrast to gemcitabine, Gemcitabine elaidate hydrochloride could be administered orally, with a schedule and dose dependent toxicity and antitumor activity.
In vitro	Gemcitabine elaidate hydrochloride, at concentrations ranging from 0.2 nM to 1 mM over 72 hours, effectively inhibits the growth of both gemcitabine-sensitive and drug-resistant cells, demonstrating IC50 values varying from 0.0015 to 91 μM across different cell lines (L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4, and MOLT4/C8, respectively). Additionally, exposure to gemcitabine elaidate (0.5 nM to 1 μM; 72 h) in A549 and WiDR cells leads to a significant increase in S phase accumulation and triggers dose-dependent cell death. Detailed cell cycle analysis of A549 and WiDR cells treated with various concentrations (0.0005 to 1.0 μM) for 72 hours confirmed the induction of G2/M and S phase accumulation.
In vivo	Gemcitabine elaidate hydrochloride, administered intraperitoneally (i.p.) at doses ranging from 25 to 120 mg/kg every three days for five doses, has demonstrated efficacy in inhibiting the growth of solid tumor xenografts in non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), and pancreatic cancer (PANC-1). Furthermore, when given orally (p.o.) at 10-20 mg/kg following the same schedule, it exhibits acceptable toxicity levels and significant antitumor activity against colon cancer xenograft in Co6044 bearing mice. A once-daily oral dose for five days shows favorable toxicity and antitumor profiles; however, a 15 mg/kg dose proves highly toxic in the same colon cancer model. Female BALB/c nude (nu/nu) mice, aged 5-8 weeks and weighing 20-27 g, served as the animal model for these experiments, bearing various tumors including EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1, and MiaPaCa-2. The treatment notably inhibited tumor growth in specific models, achieving T/C values of 7%, 1%, 30%, 7%, 9%, and 12% for EKVX, MHMX, TAX II-1, THX, CRL-1435, and PANC-1, respectively.

Synonyms	CO-101 hydrochloride, Gemcitabine elaidate hydrochloride(210829-30-4(free base)), Gemcitabine 5'-elaidate hydrochloride, CP-4126 hydrochloride
Molecular Weight	564.11
Formula	C27H44ClF2N3O5
CAS No.	2918768-08-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.64 mg/mL (10 mM), Sonication is recommended.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Clinical Compound Library NO PAINS Compound Library Bioactive Compound Library ReFRAME Related Library Nucleotide Compound Library Anti-Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gemcitabine elaidate hydrochloride 2918768-08-6 Others CP 4126 Hydrochloride CO-101 Hydrochloride Gemcitabine elaidate Hydrochloride CO101 Hydrochloride CP-4126 Hydrochloride Gemcitabine 5'-elaidate Hydrochloride CO-101 hydrochloride Gemcitabine elaidate hydrochloride(210829-30-4(free base)) CO 101 Hydrochloride CP4126 Hydrochloride Gemcitabine 5'-elaidate hydrochloride CP-4126 hydrochloride inhibitor inhibit

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