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LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $64 | In Stock | |
5 mg | $156 | In Stock | |
10 mg | $239 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $591 | In Stock | |
100 mg | $818 | In Stock | |
1 mL x 10 mM (in DMSO) | $169 | In Stock |
Description | LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity. |
In vitro | Five cell lines expressing CES2 responded to LY2334737 treatment, which was less cytotoxic to SK-OV-3 CES2 knockdown than to parental cells. CES2-transfected HCT-116 cell drug response correlated with CES2 expression level. Bystander studies showed significantly greater PC-3-GFP growth inhibition by LY2334737 when cocultured with CES2, not mock transfectants [1]. |
In vivo | Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once daily for 21 days showed significantly greater tumor growth inhibition in CES2 transfectants compared to mock transfectants (P ≤ 0.001) [1]. The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737 monotherapy (4 patients), followed by elevated transaminase levels (2 patients), both observed at the 40-50 mg dose levels. In the combination arm, 2 of 10 patients experienced DLTs at the 40 mg dose level, which included fatigue and elevated liver enzyme levels [2]. Metronomic LY2334737 administration increased blood flow in luciferase-tagged LM2-4 tumor xenografts, measurable via contrast micro-ultrasound, and coincided with a relative increase in tumor bioluminescence [3]. |
Molecular Weight | 389.39 |
Formula | C17H25F2N3O5 |
Cas No. | 892128-60-8 |
Smiles | CCCC(CCC)C(=O)Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)C2(F)F)c(=O)n1 |
Relative Density. | 1.41 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (115.56 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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