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.
CHS-828 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NYH
1.7 ± 1.2 nM
3 weeks
To determine the cytotoxicity of CHS-828 on NYH cells
BMC Cancer. 2010 Dec 12;10:677
HCT-116
12.2 ± 7.4 nM
3 weeks
To determine the cytotoxicity of CHS-828 on HCT-116 cells
BMC Cancer. 2010 Dec 12;10:677
PC-3
8.8 ± 8.4 nM
3 weeks
To determine the cytotoxicity of CHS-828 on PC-3 cells
BMC Cancer. 2010 Dec 12;10:677
human breast cancer (MCF)
18 nM
Evaluation of CHS-828 cytotoxicity against MCF cells, showing an IC50 value of 18 nM.
Molecules. 2015 Jun 23;20(6):11535-53
nasopharyngeal carcinoma (HONE1)
15 nM
Evaluation of CHS-828 cytotoxicity against HONE1 cells, showing an IC50 value of 15 nM.
Molecules. 2015 Jun 23;20(6):11535-53
human liver cancer (HEPG2)
1245 nM
Evaluation of CHS-828 cytotoxicity against HEPG2 cells, showing an IC50 value of 1245 nM.
Molecules. 2015 Jun 23;20(6):11535-53
human liver cancer (HA22T)
2067 nM
Evaluation of CHS-828 cytotoxicity against HA22T cells, showing an IC50 value of 2067 nM.
Molecules. 2015 Jun 23;20(6):11535-53
human colon cancer (DLD1)
2315 nM
Evaluation of CHS-828 cytotoxicity against DLD1 cells, showing an IC50 value of 2315 nM.
Molecules. 2015 Jun 23;20(6):11535-53
human gastric cancer (NUGC)
25 nM
Evaluation of CHS-828 cytotoxicity against NUGC cells, showing an IC50 value of 25 nM.
Molecules. 2015 Jun 23;20(6):11535-53
CCD-1064SK fibroblasts
>10 μM
72 h
Determine the IC50 value of CHS-828 for fibroblasts, showing no significant toxicity after 72 h of exposure.
J Transl Med. 2009 Mar 12;7:16
hTERT-BCE endothelial cells
50–100 nM
72 h
Determine the IC50 value of CHS-828 for endothelial cells, showing toxicity after 72 h of exposure.
J Transl Med. 2009 Mar 12;7:16
SK-N-SH cells
2–5 nM
72 h
Determine the IC50 value of CHS-828 for SK-N-SH cells, showing toxicity after 72 h of exposure.
J Transl Med. 2009 Mar 12;7:16
SH-SY5Y cells
2–5 nM
72 h
Determine the IC50 value of CHS-828 for SH-SY5Y cells, showing toxicity after 72 h of exposure.
J Transl Med. 2009 Mar 12;7:16
IMR-32 cells
0.2-0.5 nM
72 h
Evaluate the cytotoxic effects of CHS-828 on neuroblastoma cells, showing significant cell death after 72 h of exposure.
J Transl Med. 2009 Mar 12;7:16
human lymphoma cell line U-937 GTB
1.0 μM
0-48 h
To study the cytotoxic synergy and apoptosis inhibition of CHS-828 in combination with etoposide. Results showed that short pre-exposure (0-12 h) enhanced etoposide-induced caspase activation, while longer pre-exposure (18-48 h) inhibited both caspase activation and apoptotic morphology.
Br J Pharmacol. 2002 Oct;137(4):568-73
CHS-828 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Eucalyptus globulus
Eucalyptus globulus trees
Foliar spray
250 μM
Initially treated twice, then once a week after two weeks, four times in total, for 4 months
CHS-828 inhibited NAD(P)H synthesis, thereby inhibiting the OC kappa-induced increase in total essential oils and terpenoid metabolism reprogramming.
Molecules. 2014 Jun 5;19(6):7356-67
SCID mice
Orthotopic neuroblastoma model
Oral
20 mg/kg
Once daily for 10 or 30 days
Evaluate the therapeutic effects of CHS-828 on orthotopic neuroblastoma, showing significant tumor volume reduction, decreased metastasis, and no observable toxicity.
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