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PROTAK™ ARV-825
$270/ 5mg
Specification
QuantityTotal: $270
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Product Information
CAS No.1818885-28-7
Purity>98.00%
FormulaC46H47ClN8O9S
M.W.923.43
SolubilityDMSO : ≥ 50 mg/mL (54.15 mM)
Storage/StabilityStore at -20°C
BackgroundARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 uM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors.
Price270$
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