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Technical Data
| Formula | C24H24F2N8O2 |
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| Molecular Weight | 494.50 | CAS No. | 2097416-76-5 | |
| Solubility (25°C)* | In vitro | DMSO | 99 mg/mL (200.2 mM) | |
| Ethanol | 99 mg/mL (200.2 mM) | |||
| Water | 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 | AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2. | ||
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| Targets |
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| In vitro | AZD0364 exhibits high cellular potency against a direct downstream substrate on the MAPK pathway (e.g. inhibition of phospho-p90RSK1 in BRAFV600E mutant A375 cells, IC50 = 6 nM). The molecule is a highly selective kinase inhibitor (10/329 kinases tested are inhibited at >50% at a 1 µM) and has long residence time on the protein (as determined by SPR on human unphosphorylated-ERK2: pKd = 10; t1/2 = 277 mins)[2]. |
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| In vivo | AZD0364 has good oral pharmacokinetics across species. In xenograft models, AZD0364 inhibits phospho-p90RSK1 in tumors in a dose-dependent manner. AZD0364 induces regressions in the KRAS mutant NSCLC Calu 6 xenograft model. AZD0364 can also be combined safely and effectively with the MEK1/2 inhibitor selumetinib in KRAS mutant NSCLC xenograft models[2]. |
Protocol (from reference)
References
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Selleck's AZD0364 (ATG-017) has been cited by 8 publications
| Investigating the Role of TGF-β Signaling Pathways in Human Corneal Endothelial Cell Primary Culture [ Cells, 2023, 12(12)1624] | PubMed: 37371094 |
| The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] | PubMed: 37620393 |
| The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] | PubMed: 37620393 |
| The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] | PubMed: 37620393 |
| Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2 [ bioRxiv, 2023, 2023.09.12.557258] | PubMed: 37745518 |
| Non-canonical Targets of HIF1a Impair Oligodendrocyte Progenitor Cell Function [ Cell Stem Cell, 2021, 28(2):257-272.e11] | PubMed: 33091368 |
| Targeting the MAPK/ERK and PI3K/AKT Signaling Pathways Affects NRF2, Trx and GSH Antioxidant Systems in Leukemia Cells [ Antioxidants (Basel), 2020, 9(7)E633] | PubMed: 32709140 |
| Targeting the MAPK/ERK and PI3K/AKT Signaling Pathways Affects NRF2, Trx and GSH Antioxidant Systems in Leukemia Cells [ Antioxidants (Basel), 2020, 9(7):633] | PubMed: 32709140 |
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.