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首页-抗体药物偶连体和PROTACs-PROTAC-AK-1690
AK-1690

Chemical Structure : AK-1690

CAS No.: 2984505-88-4

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AK-1690 (AK1690)

货号: 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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1 mg ￥2580 In stock
5 mg ￥5880 In stock
10 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 1016.06
分子式 C51H56F2N5O11PS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

((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

参考文献

1. Kaneshige A, et al. J Med Chem. 2024 Sep 23. doi: 10.1021/acs.jmedchem.4c01009.

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