LY 345899|10538-99-5|-陌孚医药/Medlife

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LY 345899

目录号: PL07106 纯度: ≥98.0%

CAS No. :10538-99-5

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中文名称	LY 345899
英文名称	LY 345899
英文别名	LY 345899;(2S)-2-(4-(3-Amino-1,9-dioxo-1,2,5,6,6a,7-hexahydroimidazo[1,5-f]pteridin-8(9H)-yl)benzamido)pentanedioic acid;(2S)-2-[[4-(3-amino-1,9-dioxo-5,6,6a,7-tetrahydro-4H-imidazo[1,5-f]pteridin-8-yl)benzoyl]amino]pentanedioic acid;CID 9804805;E76288;A935933
Cas No.	10538-99-5
分子式	C₂₀H₂₁N₇O₇
分子量	471.42
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情	LY 345899 是一种叶酸的类似物，也是一种亚甲基四氢叶酸脱氢酶 (MTHFD1; DC301) 和 MTHFD2 抑制剂，其 IC₅₀ 值分别为 96 nM 和 663 nM，对 MTHFD1 的 K_i 值为 18 nM。
生物活性	LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC 50 values of 96 nM and 663 nM, respectively and a K i of 18 nM for MTHFD1.
性状	Solid
IC50 & Target[1][2]	Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；In solvent -80°C 6 months
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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (265.16 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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