BG45

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Technical Data

Molecular Weight 214.22 Storage powder
Formula

C11H10N4O

in solvent
CAS No. 926259-99-6 Synonyms N/A
Solubility (25°C) * In vitro DMSO 42 mg/mL (196.06 mM)
Ethanol 2 mg/mL warmed (9.33 mM)
Water Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(2-aminophenyl)pyrazine-2-carboxamide

Biological Activity

Description BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively.
Targets
HDAC3 [1]
()
HDAC1 [1] HDAC2 [1]
289 nM 2 μM 2.2 μM
In vitro BG45 causes significant cell growth inhibition and induces caspase-dependent apoptosis in a series of MM cells. In RPMI8226 cells, BG45 synergistically enhances bortezomib-induced cytotoxicity. [1]
In vivo In mice bearing MM.1S xenograft of human MM, BG45 (50 mg/kg, i.p.) significantly inhibits MM tumor growth. When in combination with bortezomib, BG45 (50 mg/kg, i.p.) enhances bortezomib-induced cytotoxicity. [1]
Features  

Protocol (Only for Reference)

Cell Assay: [1]

Cell lines MM.1S, RPMI8226, U266, H929, MM.1 R, RPMI-LR5, OPM1, OPM2 and RPMI-DOX40 cells
Concentrations ~30 μM
Incubation Time 48 h
Method The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [3H]thymidine uptake.

Animal Study: [1]

Animal Models Mice bearing MM.1S xenograft
Formulation 10% dimethylacetamide in 10% Kolliphor HS15 in PBS
Dosages 50 mg/kg, 5 days a week
Administration i.p.
 

References

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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