| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
BG45 (BG-45) is a novel, potent and selective class I HDAC inhibitor with potential anticancer activity. In cell-free experiments, it suppresses HDAC3, HDAC1, HDAC2, and HDAC6 with IC50s of 289 nM, 2.0 μM, 2.2 μM, and >20 μM, respectively. When it comes to inhibiting HDAC3, BG45 is more selective than HDAC1, 2 (IC50 = 289 nM). At IC50 >20 μM, it did not inhibit HDAC6. In a multiple myeloma mouse model, BG45 significantly reduced tumor growth when used alone or in combination with bortezomib. In MM, HDAC3 is a viable target for therapy, and the novel HDAC3 inhibitor BG45 is validated as a prototype.
| Targets |
HDAC3 ( IC50 = 0.289 μM ); HDAC1 ( IC50 = 2.0 μM ); HDAC2 ( IC50 = 2.2 μM ); HDAC6 ( IC50 > 20 μM )
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| ln Vivo |
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| Cell Assay |
The method of measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance is used to evaluate the growth inhibitory effects of BG45 in MM cell lines. [3H]thymidine uptake is used to measure the rate of DNA synthesis and, consequently, the proliferation of MM cells.
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| Animal Protocol |
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| References | |||
| Additional Infomation |
N-(2-aminophenyl)-2-pyrazinecarboxamide is an aromatic amide.
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| Molecular Formula |
C11H10N4O
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| Molecular Weight |
214.22
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| Exact Mass |
214.085
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| Elemental Analysis |
C, 61.67; H, 4.71; N, 26.15; O, 7.47
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| CAS # |
926259-99-6
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| Related CAS # |
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| PubChem CID |
16773791
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
319.0±32.0 °C at 760 mmHg
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| Flash Point |
146.7±25.1 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.708
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| LogP |
0.18
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
246
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=NC=CN=1)NC1C(N)=CC=CC=1
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| InChi Key |
LMWPVSNHKACEKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N4O/c12-8-3-1-2-4-9(8)15-11(16)10-7-13-5-6-14-10/h1-7H,12H2,(H,15,16)
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| Chemical Name |
N-(2-aminophenyl)pyrazine-2-carboxamide
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| Synonyms |
BG 45; BG-45; BG45
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6681 mL | 23.3405 mL | 46.6810 mL | |
| 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL | |
| 10 mM | 0.4668 mL | 2.3340 mL | 4.6681 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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