Apoptosis
Histone Demethylase
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Product name : ARV-825
Item : C2449
Price : 200mg, $1750;500mg, $2890; 1g, $3950;
contact : Send inquiry to: info@acesobio.com
CAS : 1818885-28-7
Molecular Weight : 923.439
Formula : C46H47ClN8O9S
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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| Details: |
Description of:ARV-825(CAS:1818885-28-7)
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. ARV-825 exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells. Co-treatment with ARV-825 and JAK inhibitor ruxolitinib was synergistically lethal against established and PD CD34+ sAML cells. Notably, ARV-825 induced high levels of apoptosis in the in vitro generated ruxolitinib-persister or ruxolitinib-resistant sAML cells. These findings strongly support the in vivo testing of the BRD4-PROTAC based combinations against post-MPN sAML. Quality control data: Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS. Product will be shipped with supporting analytical data. REFERENCES[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. |
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