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CAS No.: 200484-11-3

CHS-828 Catalog No. CSN16223

Synonyms: GMX1778

GMX1778 is a competitive NAMPT (nicotinamide phosphoribosyltransferase) inhibitor.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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.
动物研究
剂量
Mice: 25 mg/kg - 400 mg/kg^[4] (i.v.)

给药途径
i.v.

动物药代数据
Animal Mice^[4]
Dose 25 mg/kg
Administration i.v.
AUC_24h 8.46 h·μg/ml
T_1/2 2.55 h
AUC_last 8.88 h·μg/ml
C_max 0.47 μg/ml
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00724841	Metastatic Melanoma	Phase 1 Phase 2	Terminated(Study terminated pr... more >>ematurely due to financial contraints.) Collapse <<	-	United States, Pennsylvania ... more >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT00457574	Solid Tumors and Lymphomas	Phase 1	Withdrawn(Study terminated pre... more >>maturely due to financial constraints.) Collapse <<	-	-

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6892 mL
- 13.4458 mL
- 26.8916 mL
- 5 mM
- 0.5378 mL
- 2.6892 mL
- 5.3783 mL
- 10 mM
- 0.2689 mL
- 1.3446 mL
- 2.6892 mL

技术信息

CAS号

200484-11-3

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H22ClN5O

运输

蓝冰

分子量

371.86

别名

GMX1778

溶解度

DMSO	108.0 mg/mL (290.4 mM)
Water	insoluble

动物实验配方

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