Chemical Structure : AK-1690
CAS No.:
2984505-88-4
AK-1690
(AK1690)
Catalog No.: PC-23176Not For Human Use, Lab Use Only.
AK-1690 is the first, potent and selective PROTAC STAT6 degrader with DC50 of 1 nM in MV4;11 cells, Dmax>95%.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AK-1690 is the first, potent and selective PROTAC STAT6 degrader with DC50 of 1 nM in MV4;11 cells, Dmax>95%.
AK-1690 shows no significant effect on STAT1, STAT3, STAT5, and pSTAT5Y694 up to 10 μM, and modest effect on STAT2 protein at 2 and 10 μM, with a maximum reduction of STAT2 protein of <40%.
AK-1690 effectively depleted STAT6 with a DC50 value of 80 nM and a Dmax value of >90% in in human peripheral blood mononuclear cells (PBMCs).
AK-1690 effectively induces depletion of phosphorylated STAT6 (pSTAT6Y641).
AK-1690 is a potent and selective STAT6 degrader over other STAT members and >6,000 other proteins.
AK-1690 has no effect on cereblon neo-substrates IKZF1 and IKZF3, as well as IKZF2 and GSPT1, in the Jurkat cell line.
AK-1690 (200 mg/kg, i.p.) effectively depleted STAT6 protein in mouse lung and liver tissues.
Physicochemical Properties
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M.Wt
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1016.06
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Formula
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C51H56F2N5O11PS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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((2-(((2S)-1-((2S,4S)-4-((7-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)hept-6-yn-1-yl)oxy)-2-((R)-2-phenylmorpholine-4-carbonyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamoyl)benzo[b]thiophen-5-yl)difluoromethyl)phosphonic acid
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References
1. Kaneshige A, et al. J Med Chem. 2024 Sep 23. doi: 10.1021/acs.jmedchem.4c01009.
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