| Size | Price | Stock | Qty |
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| 25mg |
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Purity: ≥98%
BRD4770 (BRD-4770) is a novel and selective inhibitor of G9a (a histone methyltransferase, also known as euchromatin histone methyltransferase 2 (EHMT2)) with anticancer activity. It inhibits G9a with an IC50 of 6.3 μM, and can induce cell senescence. It exhibits excellent antiproliferative activity against various cancer cell lines such as pancreatic cancer cells-PANC-1.
| ln Vitro |
After 72 hours, PANC-1 cells treated with BRD4770 (0–20 µM) have fewer cells[1]. PANC-1 cells treated with BRD4770 (2.5–5 µM; 24 hours) have a 23% reduction in H3K9 trimethylation levels[1]. BRD4770 causes a pancreatic cancer cell line to exhibit a senescent phenotype. Moreover, BRD4770 causes G2/M cell-cycle arrest and suppresses both anchorage-dependent and -independent cell proliferation. While the ataxia telangiectasia and Rad3-related protein (ATR) pathway is unaffected, BRD4770 activates the ataxia telangiectasia mutated (ATM) route without causing DNA damage[1]. Without preventing histone deacetylases from functioning, BRD4770 also causes higher amounts of lysine acetylation in cells[1].
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| ln Vivo |
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: PANC-1 cells Tested Concentrations: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 20 µM Incubation Duration: 72 hrs (hours) Experimental Results: decreased the number of cells after 72 h. Western Blot Analysis[1] Cell Types: PANC-1 cells Tested Concentrations: 2.5 µM, 5 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished H3K9 trimethylation level by 23% in PANC-1 cells. |
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| References | |||
| Additional Infomation |
2-benzamido-1-(3-phenylpropyl)-5-benzimidazolecarboxylic acid methyl ester is a member of benzimidazoles.
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| Molecular Formula |
C25H23N3O3
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|---|---|---|
| Molecular Weight |
413.47
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| Exact Mass |
413.173
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| CAS # |
1374601-40-7
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| Related CAS # |
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| PubChem CID |
72193870
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.625
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| LogP |
5.49
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
601
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UCGWYCMPZXDHNR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H23N3O3/c1-31-24(30)20-14-15-22-21(17-20)26-25(27-23(29)19-12-6-3-7-13-19)28(22)16-8-11-18-9-4-2-5-10-18/h2-7,9-10,12-15,17H,8,11,16H2,1H3,(H,26,27,29)
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| Chemical Name |
methyl 2-benzamido-1-(3-phenylpropyl)benzimidazole-5-carboxylate
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| Synonyms |
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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 (6.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 2: 6.25 mg/mL (15.12 mM) in 0.5% Methylcellulose/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 2.4186 mL | 12.0928 mL | 24.1856 mL | |
| 5 mM | 0.4837 mL | 2.4186 mL | 4.8371 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4186 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.
Effects ofBRD4770 inhibition on the ATM and ATR pathways.ACS Chem Biol.2012 Jul 20;7(7):1152-7. |
Small-molecule inhibitors of G9a. |
Comparison of genetic and small-molecule inhibition of G9a in PANC-1 cells.ACS Chem Biol.2012 Jul 20;7(7):1152-7. |
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