SML3881
AK-2292
≥98% (HPLC)
Synonym(s):
((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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About This Item
Empirical Formula (Hill Notation):
C52H54F2N7O10PS2
CAS Number:
Molecular Weight:
1070.13
NACRES:
NA.77
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Cell penetrant, potent and highly selective degrader of STAT5A and STAT5B isoforms.
AK-2292 is a cell penetrant, potent and highly selective PROTAC degrader of STAT5A (signal transducer and activator of transcription 5 A) and STAT5B isoforms. AK-2292 potently induces degradation of STAT5 in normal mouse tissues and human chronic myeloid leukemia (CML) xenografts in mice. It potently inhibits the growth of acute myeloid leukemia (AML) cell lines.
AK-2292 is a cell penetrant, potent and highly selective PROTAC degrader of STAT5A (signal transducer and activator of transcription 5 A) and STAT5B isoforms. AK-2292 potently induces degradation of STAT5 in normal mouse tissues and human chronic myeloid leukemia (CML) xenografts in mice. It potently inhibits the growth of acute myeloid leukemia (AML) cell lines.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo
Atsunori Kaneshige
Nature Chemical Biology, 19(6), 703-711 (2023)
Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia
Journal of medicinal chemistry, 66(4), 2717-2743 (2023)
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