AK-2292 |
| Katalog-Nr.GC73203 |
AK-2292 ist ein starker und selektiver STAT5 PROTAC-Abbau mit einem DC50 von 0,10 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2984506-77-4
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
References:
[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.
[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.
| Cas No. | 2984506-77-4 | SDF | |
| Formula | C52H54F2N7O10PS2 | M.Wt | 1070.13 |
| Löslichkeit | DMSO : 125 mg/mL (116.81 mM; Need ultrasonic) | Storage | 4°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9345 mL | 4.6723 mL | 9.3447 mL |
| 5 mM | 0.1869 mL | 0.9345 mL | 1.8689 mL |
| 10 mM | 0.0934 mL | 0.4672 mL | 0.9345 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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