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Technical Data
| Formula | C20H22N2O5 |
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| Molecular Weight | 370.4 | CAS No. | 1044870-39-4 | |
| Solubility (25°C)* | In vitro | DMSO | 74 mg/mL (199.78 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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.) |
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Biological Activity
| Description | Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2. | ||
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| Targets |
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| In vitro | As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. [1] RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. [2] [3] | ||
| In vivo | RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3] | ||
| Features | First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis. |
Protocol (from reference)
| Animal Study: |
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References
Customer Product Validation
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, , BBRC, 2016, 472(4):624-630.
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Data from [Data independently produced by , , Sci Rep, 2018, 8(1):11554]
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Data from [Data independently produced by , , Acta Pharmacol Sin, 2018, doi:10.1038/s41401-018-0027-5]
Selleck's Apabetalone (RVX-208) has been cited by 19 publications
| Targeting BRD3 eradicates nuclear TYRO3-induced colorectal cancer metastasis [ Sci Adv, 2023, 9(15):eade3422] | PubMed: 37043564 |
| Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators [ Biomed Pharmacother, 2022, 152:113230] | PubMed: 35687908 |
| Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] | PubMed: 35758684 |
| Selective Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibition by the SCH772984 Compound Attenuates In Vitro and In Vivo Inflammatory Responses and Prolongs Survival in Murine Sepsis Models [ Int J Mol Sci, 2021, 22(19)10204] | PubMed: 34638546 |
| Selective Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibition by the SCH772984 Compound Attenuates In Vitro and In Vivo Inflammatory Responses and Prolongs Survival in Murine Sepsis Models [ Int J Mol Sci, 2021, 22(19)10204] | PubMed: 34638546 |
| Deletion of Glutathione S-Transferase Omega 1 Activates Type I Interferon Genes and Downregulates Tissue Factor [ Cancer Res, 2020, canres.530.2020] | PubMed: 32571799 |
| Isoform-specific Involvement of Brpf1 in Expansion of Adult Hematopoietic Stem and Progenitor Cells [ J Mol Cell Biol, 2020, 11;12(5):359-371] | PubMed: 31565729 |
| Everolimus enhances TRAIL-mediated anti-tumor activity of liver resident natural killer cells in mice [ Transpl Int, 2020, 33(2):229-243] | PubMed: 31560810 |
| Systematic Analysis of Drug Vulnerabilities Conferred by Tumor Suppressor Loss. [ Cell Rep, 2019, 27(11):3331-3344] | PubMed: 31189115 |
| Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.