[CAS NO. 200484-11-3] GMX1778 (CHS828)
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PRODUCTS SPECIFICATIONS [200484-11-3]
Store
Catalog
SLK-S8117
Brand
Selleck
CAS
200484-11-3
DESCRIPTION [200484-11-3]
Overview
| MDL | MFCD03700766 |
|---|---|
| Molecular Weight | 371.86 |
| Molecular Formula | C19H22ClN5O |
| SMILES | N#CN/C(NCCCCCCOC1=CC=C(Cl)C=C1)=N\C2=CC=NC=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL |
| 50 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL |
Description
GMX1778 (CHS828) is a potent and specific inhibitor of with and of < 25 nM and 120 nM, respectively. GMX1778 induces programmed cell death with apoptotic features. Phase 1.
In vitro
GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. GMX1778 induces programmed cell death with apoptotic features. GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM).
In vivo
GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice.
References
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