LY 345899

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY 345899 是一种叶酸类似物，也是一种亚甲基四氢叶酸脱氢酶和 MTHFD2 抑制剂（IC50 分别为 96 nM 和 663 nM，对于 MTHFD1，Ki 为 18 nM）。

LY 345899 is a Folate analog and is a methylenetetrahydrofolate dehydrogenase and MTHFD2 inhibitor (IC50: 96 nM and 663 nM, respectively and a Ki: 18 nM for MTHFD1).

LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria.LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis.

LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo. Animal Model:SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model Dosage:5-10 mg/kg Administration:Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks Result:Displayed lower cell proliferation indices and higher cell apoptosis.Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice.

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Others

Other Targets

MTHFD1

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10538-99-5

471.42

C20H21N7O7

>98% (HPLC)

DMSO:125 mg/mL (265.16 mM; Need ultrasonic)

Nc1nc(=O)c2N3C(CN(C3=O)c3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)CNc2[nH]1

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(-20℃)

With Ice Pack

≥ 2 years