详情描述
BG45 is a potent, selective and cell permeable HDAC3 inhibitor. It inhibits HDAC3 with IC50 of 289 nM. It has IC50 of 2.0 µM, 2.2 µM and >20 µM for HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. BG45 triggers significant MM cell growth inhibition via apoptosis, evidenced by caspase and poly (ADP-ribose) polymerase cleavage. BG45 alone and in combination with bortezomib triggers significant tumor growth inhibition in vivo in a murine xenograft model of human MM.
Product information
CAS Number: 926259-99-6
Molecular Weight: 214.22
Formula: C11H10N4O
Chemical Name: N-(2-aminophenyl)pyrazine-2-carboxamide
Smiles: NC1=CC=CC=C1NC(=O)C1=CN=CC=N1
InChiKey: LMWPVSNHKACEKW-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
BG45 was used at 10 µM final concentration in various in vitro assays.
In Vivo:
BG45 was dosed to mice bearing MM.1S xenograft by IP injection at 50 mg/kg (5 days a week), significantly inhibits MM tumor growth. (Formulation: 10% dimethylacetamide in 10% Kolliphor HS15 in PBS)
References:
- Minami J., et al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. (2014) Leukemia. 28(3): 680-9.
Products are for research use only. Not for human use.