GMX1778 (CHS828)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $835 | Check With Us |
| 500mg | $1350 | Check With Us |
| 1g | $2025 | Check With Us |
: Cat #: V0961 CAS #: 200484-11-3 Purity ≥ 98%
Description: GMX1778 (GMX 1778; CHS828; GMX-1778; CHS-828) is a potent and selective/specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential antitumor activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 371.86 |
|---|---|
| Molecular Formula | C19H22ClN5O |
| CAS No. | 200484-11-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 74 mg/mL (199 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | N#C/N=C(NC1=CC=NC=C1)NCCCCCCOC2=CC=C(Cl)C=C2 |
| Synonyms | CHS828; GMX-1778; CHS 828; GMX1778; CHS-828; GMX 1778 |
| Protocol | In Vitro | The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by CHS-828 (GMX1778) (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (CHS-828 (GMX1778)-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM CHS-828 (GMX1778). |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6892 mL | 13.4459 mL | 26.8918 mL | 53.7837 mL |
| 5mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | 10.7567 mL |
| 10mM | 0.2689 mL | 1.3446 mL | 2.6892 mL | 5.3784 mL |
| 20mM | 0.1345 mL | 0.6723 mL | 1.3446 mL | 2.6892 mL |
| Quality Control Documentation |
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The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.