Name | CHS-828 |
Synonyms | HS-828 CHS828 CHS 828 CHS-828 GMX 1778 GMX1778(CHS-828) 2-[6-(4-chlorophenoxy)hexyl]-1-cyano-3-pyridin-4-ylguanidine N-[6-(4-Chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinylguanidine 1-(6-(4-chlorophenoxy)hexyl)-2-cyano-3-(pyridin-4-yl)guanidine |
CAS | 200484-11-3 |
InChIKey | BOIPLTNGIAPDBY-UHFFFAOYSA-N |
Molecular Formula | C19H22ClN5O |
Molar Mass | 371.86 |
Density | 1.18±0.1 g/cm3(Predicted) |
Melting Point | 166-168°C |
Boling Point | 532.1±58.0 °C(Predicted) |
Solubility | DMSO: soluble20mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | 7.36±0.10(Predicted) |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | GMX1778 induces NAD consumption by inhibiting NAD Biosynthesis, which in turn leads to ATP depletion, ultimately leading to cell death. GMX1778 induces programmed cell death with accompanying apoptotic features. GMX1778 inhibits nuclear factor kappa B(IC50 = 8 nM) in cancer cells by down-regulating IKK activity. |
In vivo study | GMX1778 (250 mg/kg, p.o.) significant anti-tumor activity was shown for three different human neuroendocrine tumors, intestinal cancer (GOT1), pancreatic cancer (BON), and medullary thyroid cancer (GOT2). |
Hazard Symbols | T - Toxic |
Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.689 ml | 13.446 ml | 26.891 ml |
5 mM | 0.538 ml | 2.689 ml | 5.378 ml |
10 mM | 0.269 ml | 1.345 ml | 2.689 ml |
5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
biological activity | GMX1778 (CHS828) is an effective specific nicotinamide phosphoribosyltransferase (NAMPT) inhibitor, IC50 and Kd are <25 nM and 120 nM respectively. GMX1778 can induce programmed cell death with apoptotic characteristics. Phase 1. |
target | TargetValue NAMPT <25 nM NAMPT 120 nM(Kd) |
Target | Value |
NAMPT | <25 nM 120 nM(Kd) |
in vitro study | GMX1778 induce NAD consumption by inhibiting NAD biosynthesis, which subsequently leads to ATP depletion and eventually cell death. GMX1778 induces programmed cell death with apoptotic characteristics. GMX1778 inhibits nuclear factor κB(IC50=8 nM) in cancer cells by down-regulating IKK activity. |
in vivo study | in transplanted nude mice, GMX1778 (250 mg/kg, p.o.) showed significant anti-tumor activity against three different human neuroendocrine tumors, colorectal cancer (GOT1), pancreatic cancer (BON), and medullary thyroid carcinoma (GOT2). |