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Formula | C49H60ClN9O7S2 |
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Molecular Weight | 986.64 | CAS No. | 1949837-12-0 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (101.35 mM) | |
Ethanol | 100 mg/mL (101.35 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. | |||||||||||
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Targets |
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In vitro | ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis.[1] |
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In vivo | ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.[1] |
Cell Assay: |
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Animal Study: |
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Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] | PubMed: 38508142 |
Characterization of the BH1406 non-small cell lung cancer (NSCLC) cell line carrying an activating SOS1 mutation [ Transl Lung Cancer Res, 2024, 13(11):2987-2997] | PubMed: 39670010 |
ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression [ Front Pharmacol, 2022, 13:858901] | PubMed: 35600879 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.