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Technical Data
| Formula | C20H17ClF4N4O4S |
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| Molecular Weight | 520.88 | CAS No. | 1146699-66-2 | |
| Solubility (25°C)* | In vitro | DMSO | 104 mg/mL (199.66 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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Preparing Stock Solutions
Biological Activity
| Description | Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2. | ||||
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| In vitro | BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1] | ||||
| In vivo | Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). [1] | ||||
| Features | Appears to be more “notch sparing” than semagacestat (LY450139). |
Protocol (from reference)
| Animal Study:[1] |
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Customer Product Validation
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Data from [Stem Cells, 2014, 32(1), 301-12]
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Data from [Stem Cells, 2014, 32(1), 301-12]
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Data from [Data independently produced by J Biol Chem, 2014, 289(30), 20871-8]
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Data from [Data independently produced by , , Sci Rep, 2016, 6:33427]
Selleck's Avagacestat (BMS-708163) has been cited by 24 publications
| Multi-omics characterization of autophagy-related molecular features for therapeutic targeting of autophagy [ Nat Commun, 2022, 13(1):6345] | PubMed: 36289218 |
| Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
| Structural basis of γ-secretase inhibition and modulation by small molecule drugs [ Cell, 2021, 184(2):521-533.e14] | PubMed: 33373587 |
| Carboxy-terminal fragment of amyloid precursor protein mediates lipid droplet accumulation upon γ-secretase inhibition [ Biochem Biophys Res Commun, 2021, 570:137-142] | PubMed: 34280617 |
| Activation of notch 3/c-MYC/CHOP axis regulates apoptosis and promotes sensitivity of lung cancer cells to mTOR inhibitor everolimus. [ Biochem Pharmacol, 2020, 175:113921] | PubMed: 32201213 |
| A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
| RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance [ Cancer Cell, 2019, 36(1):68-83] | PubMed: 31257073 |
| EGFL7 Antagonizes NOTCH Signaling and Represents a Novel Therapeutic Target in Acute Myeloid Leukemia. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2479] | PubMed: 31672772 |
| Wild-type TP53 defined gamma-secretase inhibitor sensitivity and synergistic activity with doxorubicin in GSCs. [ Am J Cancer Res, 2019, 9(8):1734-1745] | PubMed: 31497354 |
| Iron dysregulates APP processing accompanying with sAPPα cellular retention and β-secretase inhibition in rat cortical neurons [Chen YT, et al. Acta Pharmacol Sin, 2018, 39(2):177-183] | PubMed: 28836584 |
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.