CHS-828 Property

Melting point:

166-168°C

Boiling point:

532.1±58.0 °C(Predicted)

Density 

1.18±0.1 g/cm3(Predicted)

storage temp. 

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

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

7.36±0.10(Predicted)

color 

white to beige

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.

InChIKey

BOIPLTNGIAPDBY-UHFFFAOYSA-N

Safety

Hazard Codes 

T

Risk Statements 

25-36/37/38

Safety Statements 

26-45

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CHS-828 Chemical Properties,Usage,Production

Description

CHS-828 is a pyridyl cyanoguanidine anti-tumor agent that has been identified as a competitive inhibitor of Nampt as well as an inhibitor of NF-κB pathway activity. CHS-828 has potent cytotoxic effects in human breast (IC₅₀ = 7.3 nM) and lung cancer (IC₅₀ = 0.5 nM) cells both in vitro and in vivo. In nude mice bearing human tumor xenografts, CHS-828, at 20-50 mg/kg/day, inhibits the growth of MCF-7 breast cancer tumors and induces regression of NYH small cell lung cancer tumors.

Uses

GMX1778 is an anticancer agent that inhibits cellular synthesis of NAD.

Definition

ChEBI: 2-[6-(4-chlorophenoxy)hexyl]-1-cyano-3-pyridin-4-ylguanidine is an aromatic ether.

storage

+4°C

References

1) Olesen?et al.?(2008),?Anticancer agent CHS-828 inhibits cellular synthesis of NAD; Biochem. Biophys. Res. Commun.?376?799 2) Hassan?et al. (2006),?CHS 828 kill tumor cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome; Anticancer Res.?26?4431 3) Hjarnaa?et al.?(1999),?CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo; Cancer Res.?59?5751 4) Cerna?et al.?(2012)?Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner; J. Biol. Chem.?287?22408