LY2334737
LY2334737 is an oral prodrug of gemcitabine, the clinically efficacious anticancer agent [1].
LY2334737 has been shown the hydrolytic activity by carboxylesterase 2 (CES2). The Michaelis-Menten kinetic parameters are exhibited to be : Km of 43μM and Vmax of 40nmol/min/mg protein. In addition, LY2334737 has been found to be cytotoxic to cells in the NCl-60 panel with the EC50 values of 0.512±0.016μM, 0.402±0.018μM and 0.034±0.002μM for PC-GFP alone, HCT-116 mock transfectant and HCT-116 CES2 transfectant cell lines, respectively. Apart from these, the study result has been noted that parental SK-OV-3 cells were approximately 4-fold more sensitive to LY2334737 cytotoxicity than the SK-OV-3 knockdown with the EC50 values of 1.1μM and 4.5μM, respectively [1].
References:
[1] Pratt SE1, Durland-Busbice S, Shepard RL, Heinz-Taheny K, Iversen PW, Dantzig AH. Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells. Clin Cancer Res. 2013 Mar 1;19(5):1159-68.
| Storage | Store at -20°C |
| M.Wt | 389.39 |
| Cas No. | 892128-60-8 |
| Formula | C17H25F2N3O5 |
| Solubility | Soluble in DMSO |
| Chemical Name | N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]-2-propylpentanamide |
| SDF | Download SDF |
| Canonical SMILES | CCCC(CCC)C(=O)NC1=NC(=O)N(C=C1)C2C(C(C(O2)CO)O)(F)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
