| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H43ClN5O8.Cl |
| Molecular Weight | 672.597 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Cl-].COCCOCCOCCOCCOC(=O)OC[N+]1=CC=C(NC(NCCCCCCOC2=CC=C(Cl)C=C2)=NC#N)C=C1
InChI
InChIKey=DAHMXVAETAAQOZ-UHFFFAOYSA-N
InChI=1S/C30H42ClN5O8.ClH/c1-38-16-17-39-18-19-40-20-21-41-22-23-43-30(37)44-25-36-13-10-27(11-14-36)35-29(34-24-32)33-12-4-2-3-5-15-42-28-8-6-26(31)7-9-28;/h6-11,13-14H,2-5,12,15-23,25H2,1H3,(H,33,34);1H
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C30H42ClN5O8 |
| Molecular Weight | 636.136 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
CHS-828 () is a potent and selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in the biosynthesis of NAD, which may be used to deplete cells of Nicotinamide adenine dinucleotide (NAD). Early preclinical studies revealed a high in vitro activity of CHS 828 in human tumor cell lines, a low cross-reactivity with clinically used anticancer agents, and no significant sensitivity to some of the known mechanisms of resistance. In the subsequent pharmacodynamic evaluation, CHS 828 demonstrated significant antitumor activity in several in vivo tumor models, especially pronounced in a nude mouse model of small cell lung cancer. CHS 828 exerted a high antitumor activity on eight tumor samples derived from patients with ovarian cancer and chronic lymphocytic leukemia.
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
40 or 50 or 62 mg/m2 GMX1777 (TEGLARINAD) with Temozolomide
Route of Administration:
Intravenous
U251-MG and T98 cells (5 × 10^3) were cultured in 6-well plates and treated with temozolomide alone (25, 50, 100, 200, and 400 μM), temozolomide (25, 50, 100, 200, and 400 μM) plus FK866 (5 nM and 100 nM), and temozolomide plus CHS828 (10 nM and 200 nM). At 24 hours after drug treatment, 10 μL of CCK-8 solution was added to the culture medium for 1 h at 37°C. The absorbing at 450 nm was recorded by a microplate reader and the relative cell viability was calculated.
