CHS-828

Product NameCHS-828
CAS200484-11-3
MFC19H22ClN5O
MW371.86
EINECS
MOL File200484-11-3.mol

Chemical Properties

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
pka	7.36±0.10(Predicted)
form	powder
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.
InChI	1S/C19H22ClN5O/c20-16-5-7-18(8-6-16)26-14-4-2-1-3-11-23-19(24-15-21)25-17-9-12-22-13-10-17/h5-10,12-13H,1-4,11,14H2,(H2,22,23,24,25)
InChIKey	BOIPLTNGIAPDBY-UHFFFAOYSA-N
SMILES	Clc1ccc(cc1)OCCCCCCN\C(=N\C#N)\Nc2ccncc2

Safety Information

Hazard Codes	T
Risk Statements	25-36/37/38
Safety Statements	26-45
WGK Germany	3
Storage Class	6.1C - Combustible acute toxic Cat.3 toxic compounds or compounds which causing chronic effects
Hazard Classifications	Acute Tox. 4 Oral Eye Irrit. 2 Skin Irrit. 2 STOT SE 3

Usage And Synthesis

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.

in vivo

A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of CHS-828 (GMX1778) at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. CHS-828 (GMX1778) at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg CHS-828 (GMX1778) reduced the mortality associated with toxic doses of GMX1777^[2].

storage

+4°C

References

[1] UFFE HØGH OLESEN . Anticancer agent CHS-828 inhibits cellular synthesis of NAD[J]. Biochemical and biophysical research communications, 2008, 367 4: Pages 799-804. DOI:10.1016/j.bbrc.2008.01.019
[2] SAADIA B HASSAN. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome.[J]. Anticancer research, 2006, 26 6B: 4431-4436.
[3] P J HJARNAA. CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo.[J]. Cancer research, 1999, 59 22: 5751-5757.
[4] DAVID CERNA. 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]. The Journal of Biological Chemistry, 2012: 22408-22417. DOI:10.1074/jbc.m112.357301

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