GMX1778

别名: CHS828

GMX1778是一种有效的特异性nicotinamide phosphoribosyltransferase (NAMPT)抑制剂,IC50Kd分别为 < 25 nM 和120 nM。GMX1778 可诱导具有凋亡特征的细胞程序性死亡。Phase 1。

GMX1778 Chemical Structure

GMX1778 Chemical Structure

CAS: 200484-11-3

规格 价格 库存 购买数量
10mg RMB 877.74 现货
50mg RMB 3266.15 现货
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客户使用Selleck的GMX1778发表文献6

客户使用该产品的1个实验数据

产品质控

批次: S811701 DMSO] 74 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 纯度: 99.82%
99.82

GMX1778相关产品

NAMPT抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
4T1 Antitumor assay 10 mg/kg 12 days Antitumor activity against mouse 4T1 cells implanted in BALB/c mouse assessed as reduction in tumour volume at 10 mg/kg, ip bid for 12 days by vernier caliper method 31400709
4T1 Antitumor assay 10 mg/kg 12 days Antitumor activity against mouse 4T1 cells implanted in BALB/c mouse assessed as reduction in tumor weight at 10 mg/kg, ip bid for 12 days 31400709
4T1 Antitumor assay 10 mg/kg 12 days Antitumor activity against mouse 4T1 cells implanted in Balb/c mouse mouse assessed as inhibition of tumor metastasis at 10 mg/kg, ip bid for 12 days measured post last dose by crystal violet staining based thioguanine clonogenic assay 31400709
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by SRB assay, IC50=0.005μM 23617784
NYH Cytotoxicity assay 3 weeks Cytotoxicity against human NYH cells after 3 weeks by clonogenic survival assay, LD50=0.0017μM 23679915
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis, IC50=0.005μM 23859118
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50=0.00056μM 24164086
MCF-7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50=0.0016μM 24164086
HepG2 Function assay 1 hr Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis, IC50=0.0183μM 24164086
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50=0.005μM 24405419
HONE1 Cytotoxicity assay 24 hrs Cytotoxicity against human HONE1 cells after 24 hrs by SRB assay, IC50=0.015μM 25147148
MCF Cytotoxicity assay 24 hrs Cytotoxicity against human MCF cells after 24 hrs by SRB assay, IC50=0.018μM 25147148
NUGC Cytotoxicity assay 24 hrs Cytotoxicity against human NUGC cells after 24 hrs by SRB assay, IC50=0.025μM 25147148
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50=1.245μM 25147148
HA22T Cytotoxicity assay 24 hrs Cytotoxicity against human HA22T cells after 24 hrs by SRB assay, IC50=2.067μM 25147148
DLD1 Cytotoxicity assay 24 hrs Cytotoxicity against human DLD1 cells after 24 hrs by SRB assay, IC50=2.315μM 25147148
A2780 Function assay 72 hrs Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay, IC50=0.001μM 27541271
Rosetta (DE3) Function assay 15 mins Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP, IC50=0.002μM 27541271
PC3 Antiproliferative assay 5 days Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay, IC50=0.0044μM 28610984
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 GMX1778是一种有效的特异性nicotinamide phosphoribosyltransferase (NAMPT)抑制剂,IC50Kd分别为 < 25 nM 和120 nM。GMX1778 可诱导具有凋亡特征的细胞程序性死亡。Phase 1。
靶点
NAMPT [1] NAMPT [1]
<25 nM 120 nM(Kd)
体外研究(In Vitro)
体外研究活性 GMX1778通过抑制NAD+生物合成诱导NAD+消耗,随后导致ATP耗竭,最终使细胞死亡。[1] GMX1778诱导程序性细胞死亡,并伴随凋亡特征。[2] GMX1778通过下调IKK活性,抑制癌症细胞中核因子κB(IC50=8 nM)。[3]
激酶实验 体外耦合酶 NAMPT 试验
重组NAMPT活性使用基于NAD+定量的耦合酶测定进行评估。反应在室温下使用包含50 mM HEPES (pH 7.4),50 mM KCl,5 mM MgCl2,0.5 mM β-巯基乙醇,0.005% 牛血清白蛋白,1% DMSO,2.0 U/ml乳酸脱氢酶,4 mM L-乳酸钠,0.4 U/ml 心肌黄酶,6 μΜ 刃天青钠盐,0.4 mM PRPP,3.0 nM NMNAT1,125 μM ATP,50 μM NM,和2-5 μM 重组NAMPT的混合物进行180分钟。荧光性使用Tecan Safire酶标仪(激发波长560 nm;发射波长590 nm)测量。Ki值使用Graphpad Prism 4.0软件和Cheng-Prusoff方程计算。
细胞实验 细胞系 HeLa 细胞
浓度 ~100 nM
孵育时间 72小时
方法 GMX1778在DMSO中连续稀释以达到0.2% DMSO的终浓度。72小时后,相对ATP水平使用ViaLight HS高灵敏度细胞毒性和细胞增殖生物测定试剂盒根据制造商指示测定。对于GMX1778细胞毒性挽救实验,细胞用NA (10 μM)或NMN (100 μM)处理,同时使用GMX1778处理。S形剂量响应曲线使用4.00版 GraphPad Prism(GraphPad 软件) 通过可变斜率的非线性回归分析生成,以计算50%抑制(IC50)值。
体内研究(In Vivo)
体内研究活性 在移植的裸鼠体内,GMX1778 (250 mg/kg, p.o.)对三种不同的人神经内分泌肿瘤,肠癌(GOT1),胰腺癌(BON),和甲状腺髓样癌(GOT2)表现出显著的抗肿瘤活性。[4]
动物实验 Animal Models 负荷中肠癌(GOT1),胰腺癌(BON)和甲状腺髓样癌(GOT2)肿瘤的裸鼠
Dosages ~250 mg/kg
Administration p.o.

化学信息&溶解度

分子量 371.86 分子式

C19H22ClN5O

CAS号 200484-11-3 SDF Download GMX1778 SDF
Smiles C1=CC(=CC=C1OCCCCCCN=C(NC#N)NC2=CC=NC=C2)Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 74 mg/mL ( 198.99 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
Could you please suggest me the suitable formulation of S8117 for in vivo study?

回答:
You can dissolve S8117 in 1%CMC-Na (suspension) for oral administration.

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