2. PROTAC JAK/STAT Signaling Stem Cell/Wnt
  3. PROTACs STAT
  4. AK-2292

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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AK-2292 Chemical Structure

AK-2292 Chemical Structure

CAS No. : 2984506-77-4

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Description

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.

IC50 & Target[1]

STAT5

0.10 μM (DC50)

In Vitro

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.

AK-2292 Related Antibodies

Western Blot Analysis[1]

Cell Line: SKNO1 cells
Concentration: 0.008, 0.04, 0.2, 1, 5 μM
Incubation Time: 18 hours
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.

Cell Viability Assay[1]

Cell Line: SKNO1, MV4;11, and Kasumi-3 cells
Concentration: 0.0015, 0.015, 0.15, 1.5, 15 μM
Incubation Time: 4 days
Result: Effectively inhibited cell growth with IC50s of 0.36, 0.18, and 0.35 μM, respectively.
In Vivo

AK-2292 (50-200 mg/kg; i.p. once a day, 5 days a week for 3 weeks) inhibits tumor growth in the MV4;11 xenograft model in mice[1].
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.

Animal Model: SCID mice bearing MV4;11 tumors[1]
Dosage: 50, 100, 200 mg/kg
Administration: I.p. injection, once a day, 5 days per week for 3 weeks
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.
Molecular Weight

1070.13

Formula

C52H54F2N7O10PS2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Purity & Documentation

Purity: 99.73%

SDS (252 KB)

COA (248 KB) HNMR (230 KB) CNMR (255 KB) RP-HPLC (156 KB) MS (112 KB)

Handling Instructions (2659 KB)
References
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AK-2292 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AK-22922984506-77-4AK2292AK 2292PROTACsSTATSTAT5PROTACSTAT5ASTAT5B acute myeloid leukemiachronic myeloid leukemiacancerInhibitorinhibitorinhibit

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