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Chemical Structure : AK-2292
CAS No.: 2984506-77-4
Catalog No.: PC-49629Not For Human Use, Lab Use Only.
AK-2292 (AK2292) is a first, potent and selective small-molecule degrader of both STAT5A and STAT5B isoforms.
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AK-2292 (AK2292) is a first, potent and selective small-molecule degrader of both STAT5A (Ki=210 nM) and STAT5B (Ki=308 nM) isoforms.
AK-2292 effectively induces degradation of STAT5A, STAT5B, and phosphorylated STAT5 proteins in a concentration- and time-dependent manner in acute myeloid leukemia (AML) cell lines.
AK-2292 demonstrates excellent degradation selectivity for STAT5 over all other STAT members.
AK-2292 exerts potent and specific cell growth inhibitory activity in AML cell lines with high levels of phosphorylated STAT5.
AK-2292 effectively induces STAT5 depletion in normal mouse tissues and human chronic myeloid leukemia (CML) xenograft tissues and achieves tumor regression in CML xenograft mouse models.
| M.Wt | 1070.13 | |
| Formula | C52H54F2N7O10PS2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
((2-(((2S)-1-((2S)-2-((3-((5-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)(methyl)amino)-3-oxopropyl)(4-(thiazol-2-yl)phenyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamoyl)benzo[b]thiophen-5-yl)difluoromethyl)-phosphonic Acid |
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1. Kaneshige A,et al. Nat Chem Biol. 2023 Feb 2. doi: 10.1038/s41589-022-01248-4.
2. Kaneshige A, et al. J Med Chem. 2023 Feb 3. doi: 10.1021/acs.jmedchem.2c01665.
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