Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $185 | In Stock | |
50 mg | $337 | In Stock | |
1 mL x 10 mM (in DMSO) | $79 | In Stock |
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. |
Alias | 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) ![]() | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.