货号	规格	价格	上海	北京	珠海	重庆	武汉
S89140-5mg买3赠1	98.00%	￥690.00 S89140-5mg ￥690.00 现货（买3赠1）	4 4	-	-	-	-
S89140-10mg促销	98.00%	￥1180.00 ￥944.00 S89140-10mg ￥944.00 现货	4 4	-	-	-	-
S89140-25mg促销	98.00%	￥2520.00 ￥2010.00 S89140-25mg ￥2010.00 现货	4 4	-	-	-	-
S89140-100mg促销	≥98%	￥6480.00 ￥5180.00 S89140-100mg ￥5180.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1

靶点：

Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2);DHFR

体外研究：

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。

体内研究：

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.

参考文献：

1. Schmidt A, et al. Structures of three inhibitor complexes provide insight into the reaction mechanism of the human methylenetetrahydrofolate dehydrogenase/cyclohydrolase. Biochemistry. 2000 May 30;39(21):6325-35. 2. Tedeschi PM, et al. Mitochondrial Methylenetetrahydrofolate Dehydrogenase (MTHFD2) Overexpression Is Associated with Tumor Cell Proliferation and Is a Novel Target for Drug Development. Mol Cancer Res. 2015 Oct;13(10):1361-6. 3. Gustafsson R, et al. Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor. Cancer Res. 2017 Feb 15;77(4):937-948. 4. Huai-Qiang Ju, et al.Modulation of Redox Homeostasis by Inhibition of MTHFD2 in Colorectal Cancer: Mechanisms and Therapeutic Implications. J Natl Cancer Inst. 2019 Jun 1;111(6):584-596.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.121 ml	10.606 ml	21.213 ml
5 mM	0.424 ml	2.121 ml	4.243 ml
10 mM	0.212 ml	1.061 ml	2.121 ml
50 mM	0.042 ml	0.212 ml	0.424 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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