CO-101 (CP-4126) Inhibitor CAS No. 210829-30-4

Cat. No.	Name	Size	Price
KI2631	CO-101 (CP-4126)	20 mg	$494
	CO-101 (CP-4126)	50 mg	$1170
	CO-101 (CP-4126)	100 mg	$1950
	CO-101 (CP-4126)	200 mg	$2990

Chemical Characteristic

Product Name	CO-101 (CP-4126)
Synonyms	Gemcitabine elaidate; CP-4126
CAS No.	210829-30-4
Molecular Weight	527.6
Formula	C₂₇H₄₃F₂N₃O₅
Chemical Name	(E)-((2R,3R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-4,4-difluoro-3-hydroxytetrahydrofuran-2-yl)methyl octadec-9-enoate.
Smiles	c1(=O)nc(ccn1C1O[C@@H]([C@H](C1(F)F)O)COC(=O)CCCCCC/C=C/CCCCCCCCC)N
Chemical Structure

Biological activities

CO-101 is a lipophilic and unsaturated fatty acid ester derivative of gemcitabine (dFdC). CO-101 is an antimetabolite deoxynucleoside analogue, showing potential antineoplastic activity. CO-101 is active in ara-C and gemcitabine resistant lymphoma cell lines.^[1] In vitro, CO-101 shows a nucleoside-transporter independent uptake, with long retention of the active nucleotides in leukemic CEM-cell-line.^[2] In vitro, CO-101 also increases the accumulation of oxaliplatin (OHP) in the WiDR cell line with 40%, and enhances docetaxel induced cell kill.^[3] In melanoma, sarcoma, lung, prostate, pancreatic and breast cancer xenografts models, CP-4126 displays potent antitumor activities as well as gemcitabine. In the non-small cell lung cancer xenografts EKVX, CO-101 treatment at dose of 20 mg/kg increases both the antitumor effect and the toxicity. In the non-small cell lung cancer xenografts MAKSAX, CO-101 treatment at dose of 22.5 mg/kg five times every 3 days causes acceptable toxicity with a good antitumor effect.^[4]

Protocols

In vitro: CO-101 is dissolved in dimethyl sulfoxide (DMSO).^[4]

References

[1] Galmarini CM, et al. CP-4055 and CP-4126 are active in ara-C and gemcitabine-resistant lymphoma cell lines. Br J Haematol. 2009, 144(2): 273-275. [2] Adema AD, et al. Metabolism and accumulation of the lipophilic deoxynucleoside analogs elacytarabine and CP-4126. Invest New Drugs. 2012, 30(5): 1908-1916. [3] AD Adema, et al. The fatty acid derivatives of Ara-C, CP-4055, and gemcitabine, CP-4126, enhance the cytotoxic effect of oxaliplatin and docetaxel. 2006, Proc Amer Assoc Cancer Res. [4] 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, 29(3): 456-466.

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