2984506-77-4
Chemical Structure
AK-2292
- CAS No.: 2984506-77-4
- Formula:C52H54F2N7O10PS2
- Molecular Weight:1070.13
IUPAC Name: (2R,3R,4S,5R)-5-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-fluoro-2-(hydroxymethyl)tetrahydrofuran-3-ol
InChIKey: LOPYPDQOHNOVBM-QOIUHGAOSA-N
SMILES: FC(C1=CC=C2C(C=C(C(N[C@@H](C(C)(C)C)C(N3[C@H](C(N(CCC(N(CCCC#CC4=CC=CC5=C4CN(C(CC6)C(NC6=O)=O)C5=O)C)=O)C7=CC=C(C8=NC=CS8)C=C7)=O)CCC3)=O)=O)S2)=C1)(P(O)(O)=O)F
Biological Activity: AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models[1][2]. AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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AK-2292 | 98.96% | AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | ||||||||||||||||||||
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- [1]. Kaneshige A, et, al. Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia. J Med Chem. 2023 Feb 3. [Content Brief]
- [2]. Kaneshige A, et, al. A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo. Nat Chem Biol. 2023 Feb 2. [Content Brief]
Keywords
