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CHS-828

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Chemical Structure| 200484-11-3 同义名 : GMX1778
CAS号 : 200484-11-3
货号 : A215361
分子式 : C19H22ClN5O
纯度 : 98%
分子量 : 371.864
MDL号 : MFCD03700766
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(107.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • NAMPT

    NAMPT, IC50:<25 nM

    NAMPT, Kd:120 nM
描述 NAMPT (nicotinamide phosphoribosyltransferase) is a crucial factor in the resynthesis of NAD. GMX1778 is a NAMPT inhibitor. GMX1778 at 10nM led a dramatic drop in NAD levels of NYH cells post 24h. GMX1778 exerted potent cytotoxic effects in human breast and lung cancer cell lines, with lesser effects on normal fibroblasts and endothelial cells. Oral administration of GMX1778 at dose ranging in 20-50mg/kg inhibited the growth of MCF-7 breast cancer tumors and caused regression of NYH small cell lung cancer tumors in nude mice bearing human tumor xenografts.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.45mL

2.69mL

1.34mL

26.89mL

5.38mL

2.69mL
参考文献

[1]Karpov AS, Abrams T, et al. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842.

[2]Olesen UH, Christensen MK, et al. Anticancer agent CHS-828 inhibits cellular synthesis of NAD. Biochem Biophys Res Commun. 2008 Mar 21;367(4):799-804.

[3]Hjarnaa PJ, Jonsson E, et al. CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo. Cancer Res. 1999 Nov 15;59(22):5751-7.

[4]Beauparlant P, Bédard D, et al. Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. 2009 Jun;20(5):346-54.