| Chemical Properties | Back Directory | [density ]
1.41±0.1 g/cm3(Predicted) | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Solid | [pka]
10.81±0.40(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Description]
JQAD1 is a potent and selective EP300 Degrader | [Uses]
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer[1]. | [in vivo]
JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts[1]. | Animal Model: | NSG mice with Kelly NB cell xenografts[1] | | Dosage: | 40 mg/kg | | Administration: | Intraperitoneal injection; daily, for 21 days | | Result: | Suppressed tumor growth and prolonged survival. |
| Animal Model: | CD1 mice[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection (Pharmacokinetic Analysis) | | Result: | Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L. |
| [storage]
Store at -20°C | [References]
[1] Durbin AD, et, al. EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma. Cancer Discov. 2022 Mar 1;12(3):730-751. DOI:10.1158/2159-8290.CD-21-0385 |
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