LY2334737

产品编号: DC9304 Featured
LY2334737
结构式
892128-60-8
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中国地区超过5000个高品质化合物库存
应用领域
LY2334737是口服活性的gemcitabine原药。
Cas No.: 892128-60-8
名称:
别名: LY 2334737,LY-2334737,LY2334737
SMILES: CCCC(CCC)C(=O)NC1=NC(=O)N(C=C1)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F
分子式: C17H25F2N3O5
分子量: 389.39
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy. IC50 Value: 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. 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). 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. 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_2628_DC9304_892128-60-8
COA
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