GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. GSK1324726A inhibits cell growth and induces cytotoxicity in neuroblastoma cell lines. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN.
In vivo, in the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. [1] In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals.
Cell Experiment | |
---|---|
Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
---|---|
Animal models | Xenograft models of non-MYCN-amplified and MYCN-amplified neuroblastoma in immunocompromised mice using the SK–N-AS and CHP-212 cell lines |
Formulation | Suspended in 1% methylcellulose |
Dosages | 15 mg/kg once daily |
Administration | p.o. |
Molecular Weight | 434.91 |
Formula | C25H23ClN2O3 |
CAS Number | 1300031-52-0 |
Solubility (25°C) | DMSO: ≥ 43 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Epigenetic Reader Domain Products |
---|
Phoenixin-20
Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. |
Menin-MLL inhibitor 31
Menin-MLL inhibitor 31 is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM. |
OPN-2853
OPN-2853 is a bromodomain protein-4 (BRD4) inhibitor that can be used in studies related to hematologic and lymphatic disorders. |
HDAC/JAK/BRD4-IN-1
HDAC/JAK/BRD4-IN-1 is a potent HDAC/JAK/BRD4 triple inhibitor. |
VYN-201
VYN-201 is a novel pan-BET inhibitor for studies related to idiopathic pulmonary fibrosis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.