CP-4126 (LVT derivative of Gemcitabine)
CP-4126 (LVT derivative of Gemcitabine) Basic information
- Product Name:
- CP-4126 (LVT derivative of Gemcitabine)
- Synonyms:
-
- CP-4126 (LVT derivative of Gemcitabine)
- CP 4126
- GeMcitabine 5'-elaidate
- GeMcitabine elaidate
- Gemcitabine elaidate(CP-4126
- CO-101:CP-4126:Gemcitabineelaidate
- CO-101; CO101; CO 101; CP-4126; CP4126; CP 4126; GEMCITABINE ELAIDATE
- CS-1569
- CAS:
- 210829-30-4
- MF:
- C27H43F2N3O5
- MW:
- 527.64
- Mol File:
- 210829-30-4.mol
CP-4126 (LVT derivative of Gemcitabine) Chemical Properties
- Boiling point:
- 631.4±65.0 °C(Predicted)
- Density
- 1.20±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Ethanol:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.63(Max Conc. mM)
DMSO:28.0(Max Conc. mg/mL);53.07(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);56.86(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);56.86(Max Conc. mM) - form
- A crystalline solid
- pka
- 11.48±0.70(Predicted)
- color
- White to off-white
CP-4126 (LVT derivative of Gemcitabine) Usage And Synthesis
Uses
Gemcitabine elaidate (CP-4126) is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity[1][2].
Definition
ChEBI: Gemcitabine elaidate is a pyrimidine 2'-deoxyribonucleoside.
in vivo
Gemcitabine 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)[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[1].
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[1].
| 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[1] |
| 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. |
References
[1] Bergman AM, et, al. 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
[2] Adema AD, et, al. 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. PMID:19956857
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