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.
(Pink: STAT5 ligand (HY-184991); Blue: Cereblon ligand (HY-43722); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.28%
- CAS 番号: 2984506-77-4
- 分子式: C52H54F2N7O10PS2
- 分子量:1070.13
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 AK-2292
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生物活性
製品説明
IC50 & Target
[1]|
STAT5 0.10 μM (DC50) |
Cellular Effect
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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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 2984506-77-4
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性状 Solid
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分子量 1070.13
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 -
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (46.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (1.17 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (288 KB)
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SDS (252 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9345 mL | 4.6723 mL | 9.3447 mL | 23.3616 mL |
| 5 mM | 0.1869 mL | 0.9345 mL | 1.8689 mL | 4.6723 mL | |
| 10 mM | 0.0934 mL | 0.4672 mL | 0.9345 mL | 2.3362 mL | |
| 15 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5574 mL | |
| 20 mM | 0.0467 mL | 0.2336 mL | 0.4672 mL | 1.1681 mL | |
| 25 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9345 mL | |
| 30 mM | 0.0311 mL | 0.1557 mL | 0.3115 mL | 0.7787 mL | |
| 40 mM | 0.0234 mL | 0.1168 mL | 0.2336 mL | 0.5840 mL |
AK-2292 関連分類
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