GMX1778
别名: CHS828
GMX1778是一种有效的特异性nicotinamide phosphoribosyltransferase (NAMPT)抑制剂，IC50 和 Kd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
CAS: 200484-11-3
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GMX1778相关产品
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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，IC50 和 Kd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 |
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| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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] |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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