| Name | ARV-771 |
| Description | ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM. |
| In vitro | METHODS: ARV-771 (0.01/0.025/0.05/0.1/0.25/0.5/1/2μM) was used to culture Hep3B, HepG and HCCLM3 cells to observe whether ARV-771 inhibits the growth of these cancer cells.
RESULTS ARV-771 had a dose-dependent inhibition on cancer cell viability when the concentration reached 0.25 μM in Hep3B and HepG2 cells and 0.5 μM in HCCLM3 cells. [1] |
| In vivo | METHODS: Nude mice successfully bearing transplanted HepG2 cell tumors were randomly divided into two groups and treated with ARV-771 (20 mg/kg/day, subcutaneous injection) every other day for 25 days. Tumor volume and body weight of mice were measured every 5 days. Immediately after extraction of xenografts from mice, tumor weight was measured by an electronic balance.
RESULTS After ARV-771 treatment, tumor volume and tumor weight were significantly reduced. Immunochemical detection results showed that ARV-771 reduced the expression of Ki67 and increased the expression of cleaved Caspase 3 in xenograft tissues. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (2.03 mM), Sonication is recommended.
DMSO : 250 mg/mL (253.39 mM), Sonication is recommended.
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| Keywords | PROTACs | Inhibitor | inhibit | EpigeneticReaderDomain | Epigenetic Reader Domain | BET | ARV-771 | ARV771 | ARV 771 |
| Inhibitors Related | ABBV-744 | SNDX-5613 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Bavdegalutamide | Curcumin | Naphthol AS-E | Vepdegestrant | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
