Daprodustat (GSK1278863)

Catalog No.S8171 Batch:S817101

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Technical Data

Formula

C19H27N3O6
Molecular Weight 393.43 CAS No. 960539-70-2
Solubility (25°C)* In vitro DMSO 10 mg/mL (25.41 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.125mg/ml Taking the 1 mL working solution as an example, add 50 μL of 2.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

Description Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.
Targets
HIF-PH [1]
In vitro GSK1278863 induces an effective EPO response and stimulates non-EPO mechanisms for erythropoiesis. [1]

Protocol (from reference)

Selleck's Daprodustat (GSK1278863) has been cited by 4 publications

Pharmacologic HIF stabilization activates costimulatory receptor expression to increase antitumor efficacy of adoptive T cell therapy [ Sci Adv, 2024, 10(35):eadq2366] PubMed: 39196939
Hypoxic and pharmacological activation of HIF inhibits SARS-CoV-2 infection of lung epithelial cells [ Cell Rep, 2021, 35(3):109020] PubMed: 33852916
HIF hydroxylase inhibitors decrease cellular oxygen consumption depending on their selectivity. [ FASEB J, 2020, 34(2):2344-2358] PubMed: 31908020
Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers [ Cancer Res, 2019, 79(10):2564-2579] PubMed: 30898838

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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.