BG45 |
| Catalog No.GC12074 |
Novel HDAC3-selective inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 926259-99-6
Sample solution is provided at 25 µL, 10mM.
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Description:
IC50: 289 nM
Histone deacetylases (HDACs) represent novel molecular targets for the treatment of various types of cancers including multiple myeloma (MM). Many HDAC inhibitors have already shown remarkable anti-tumor activities in the preclinical studies, however, their clinical utility is limited due to unfavorable toxicities associated with their broad range HDAC inhibitory effects. BG45 is a novel small molecule HDAC3-selective inhibitor.
In vitro: BG45 is reported as an HDAC class I inhibitor with selectivity for HDAC3 over HDAC1, 2. Consistent with HDAC3 knockdown data, BG45 significantly inhibited MM cell growth dose-dependently. Importantly, BG45 also triggered a potent growth inhibitory effect against patient-derived MM cells, without affecting normal donor PBMCs [1].
In vivo: BG45 significantly inhibited MM tumor growth in a dose-dependent fashion. For example, significant differences were observed in control versus BG45 15 mg/kg, control versus BG45 50 mg/kg, and BG45 15 mg/kg versus BG45 50 mg/kg at day 22. Moreover, BG45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. These results confirmed that BG45 triggers in vivo anti-MM activities [1].
Clinical trial: Up to now, BG45 is still in the preclinical development stage.
Reference:
[1] Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KC. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.
| Cas No. | 926259-99-6 | SDF | |
| Chemical Name | (Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid | ||
| Canonical SMILES | NC1=CC=CC=C1/N=C(O)/C2=CN=CC=N2 | ||
| Formula | C11H10N4O | M.Wt | 214.22 |
| Solubility | DMF: 5 mg/ml,DMSO: 30 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 3 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.6681 mL | 23.3405 mL | 46.681 mL |
| 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL |
| 10 mM | 0.4668 mL | 2.334 mL | 4.6681 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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