AK-2292
Based on 2 publication(s) in Google Scholar
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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- Reinheit: 98.96%
- CAS. Nr.: 2984506-77-4
- Formel: C52H54F2N7O10PS2
- Molecular Weight:1070.13
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AK-2292
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Biologische Aktivität
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STAT5 0.10 μM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
>15 μM
Compound: AK-2292
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Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
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[PMID: 36735833] |
| MOLM-13 | IC50 |
>15 μM
Compound: AK-2292
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Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
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[PMID: 36735833] |
| MV4-11 | IC50 |
0.18 μM
Compound: AK-2292
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Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
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[PMID: 36735833] |
| OCI-AML2 | IC50 |
>15 μM
Compound: AK-2292
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Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
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[PMID: 36735833] |
| RS4-11 | IC50 |
>15 μM
Compound: AK-2292
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Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition measured for 4 days by celltiter-glo assay
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[PMID: 36735833] |
AK-2292 (0.0015-15 μM; 4 days) inhibits the cell growth of SKNO1, MV4;11, and Kasumi-3 cells, with IC50s of 0.36, 0.35, and 0.18 μM, respectively[1].
AK-2292 (0.008-5 μM; 18 h) reduces the levels of STAT5A, STAT5B and pSTAT5Y694 proteins in the SKNO1 cell line[1].
AK-2292 (0.008-5 μM; 6 h) effectively reduces the levels of STAT5 and pSTAT5Y694 in the MV4;11 acute leukemia cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKNO1 cells
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Concentration:0.008, 0.04, 0.2, 1, 5 μM
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Incubation Time:18 hours
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Result:Reduced the levels of STAT5A, STAT5B, and pSTAT5Y694 by >75% at 0.2 μM and by >95% at 1 μM.
Has no obvious effect on the levels of STAT1, STAT2, STAT3, STAT4, and STAT6 proteins at concentrations up to 5 μM.
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Cell Line:SKNO1, MV4;11, and Kasumi-3 cells
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Concentration:0.0015, 0.015, 0.15, 1.5, 15 μM
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Incubation Time:4 days
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Result:Effectively inhibited cell growth with IC50s of 0.36, 0.18, and 0.35 μM, respectively.
AK-2292 (150 mg/kg; a single i.p.) induces rapid and >95% depletion of STAT5 and pSTAT5Y694 proteins in the MV4;11 xenograft tissues in mice[1].
AK-2292 (i.p.) exhibits good plasma exposure and has a plasma half-life of 1.9 h, moderate clearance (CL=0.77 L/h/kg), and good volume distribution (Vz=2.1 L/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice bearing MV4;11 tumors[1]
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Dosage:50, 100, 200 mg/kg
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Administration:I.p. injection, once a day, 5 days per week for 3 weeks
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Result:Inhibited tumor growth in a dose-dependent manner and achieved 50, 60, and 80% of tumor growth inhibition at doses of 50, 100, and 200 mg/kg, respectively.
Did not induce animal weight loss or any other signs of toxicity.
Chemical Information
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CAS. Nr. 2984506-77-4
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Appearance Solid
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Molecular Weight 1070.13
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Formel C52H54F2N7O10PS2
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Color Off-white to light yellow
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
BCR::ABL1-Induced Enhancer Reprogramming Uncovers Hypersensitivity of Ph+B-ALL Cells to Enhancer-Targeting Drugs. [Abstract]2026 Mar 1:e17231. PMID: 41764406 -
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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