Mocetinostat (MGCD0103)
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 |
|---|---|---|
| 500mg | $330 | Check With Us |
| 1g | $560 | Check With Us |
| 5g | $1680 | Check With Us |
: Cat #: V0259 CAS #: 726169-73-9 Purity ≥ 98%
Description: Mocetinostat (formerly MGCD-0103 or MG-0103), is a potent, benzamide-based and orally bioavailable Class I-selective inhibitor of human histone deacetylases (HDAC) with potentianl anticancer activities.
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| Molecular Weight (MW) | 396.44 |
|---|---|
| Molecular Formula | C23H20N6O |
| CAS No. | 726169-73-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 13 mg/mL (32.8 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL |
| Synonyms | MG0103; MG-0103; MG 0103; MGCD0103; MGCD 0103; MGCD-0103 |
| Protocol | In Vitro | Mocetinostat is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8. Mocetinostat (MGCD0103) exhibits potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro, and HDAC inhibitory activity is required for these effects. In all cell lines tested, Mocetinostat (MGCD0103) partially inhibits cellular HDAC enzyme activity although the maximal inhibition of activity varies among cell lines from 75% to 85% of total activity. The IC50 of Mocetinostat in intact cancer cells is independent of tissue origin. In A549 cells, MGCD0103 shows dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, Mocetinostat inhibits a maximum of 80% of total activity. In HCT116 cells, Mocetinostat induces a significant S-phase depletion and both G1 and G2-M accumulation |
|---|---|---|
| In Vivo | Mocetinostat (MGCD0103) significantly inhibits growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors. The p.o. administration of Mocetinostat (MGCD0103) (2HBr salt) significantly reduces growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. Mocetinostat (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocks growth of tumors compared with vehicle treatment alone (P<0.05 in post-ANOVA Dunnett's test) with no change in body weight |
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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | 50.4490 mL |
| 5mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | 10.0898 mL |
| 10mM | 0.2522 mL | 1.2612 mL | 2.5224 mL | 5.0449 mL |
| 20mM | 0.1261 mL | 0.6306 mL | 1.2612 mL | 2.5224 mL |
The molarity calculator equation
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
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,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.