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LY2334737

Catalog No. T4061 CAS 892128-60-8

LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.

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LY2334737, CAS 892128-60-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 91.00
2 mg	In stock	$ 132.00
5 mg	In stock	$ 198.00
10 mg	In stock	$ 297.00
25 mg	In stock	$ 497.00
50 mg	In stock	$ 716.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 198.00

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Purity: 100%

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Description	LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.
In vitro	Five cell lines that express CES2 responded to LY2334737treatment. LY2334737 was less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies showed statistically greater PC-3-GFP growth inhibition by LY2334737 when cells were cocultured with CES2 and not mock transfectants [1].
In vivo	Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days showed greater tumor growth inhibition of CES2 transfectant than the mock transfectant (P ≤ 0.001) [1]. The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737monotherapy (4 patients) followed by elevated transaminase levels (2 patients), both observed at the 40- to 50-mg dose levels. Among the 10 patients in the combination arm, 2 had DLTs at the 40-mg dose level. These were fatigue and elevated liver enzyme levels [2]. Metronomic LY2334737 administration caused increased blood flow in luciferase-tagged LM2-4 tumor xenografts, and this effect, readily measured using contrast micro-ultrasound, coincided with a relative increase in tumor bioluminescence [3].

Molecular Weight	389.39
Formula	C17H25F2N3O5
CAS No.	892128-60-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (115.56 mM)

References and Literature

1. Pratt SE, et al. 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. 2. Koolen SL, et al. Phase I study of Oral gemcitabine prodrug (LY2334737) alone and in combination with erlotinib in patients with advanced solid tumors. Clin Cancer Res. 2011 Sep 15;17(18):6071-82. 3. Francia G, et al. Low-dose metronomic oral dosing of a prodrug of gemcitabine (LY2334737) causes antitumor effects in the absence of inhibition of systemic vasculogenesis. Mol Cancer Ther. 2012 Mar;11(3):680-9. 4. Cai Y, Zhou H, Zhu Y, et al. Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice[J]. Cell Research. 2020: 1-16.

Citations

1. Cai Y, Zhou H, Zhu Y, et al. Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice. Cell Research. 2020: 1-16.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Viral Compound Library Bioactive Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library Orally Active Compound Library NO PAINS Compound Library

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Keywords

LY2334737 892128-60-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Others Virus Protease Nucleoside Antimetabolite/Analog anticancer LY-2334737 HEV Gemcitabine HEVs HRVs EV-A71 Rhinovirus inhibit LY 2334737 Enterovirus HRV orally antiviral Inhibitor inhibitor

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