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| 5mg |
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Purity: ≥98%
AI-10-49 is a potent and selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient with AI-10-49 triggers selective cell death. Direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers. The stability of RUNX1, CBFb, and CBFb-SMMHC was not affected by AI-10-49.
| ln Vitro |
AI-10-49, with an IC50 value of 0.26 μM, blocks CBFβ-SMMHC from binding to the RUNX1 Runt domain [1]. AI-10-49 (1 μM; 3, 6, 12 hours) reduces CBFβ-SMMHC binding to RUNX1 in a specific manner[1].
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| ln Vivo |
Leukemia in mice is delayed in its progression by AI-10-49 (200 mg/kg; daily) [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: ME-1 cells Tested Concentrations: 1 μM Incubation Duration: 3, 6 hrs (hours) Experimental Results: Effectively dissociated RUNX1 from CBFβ-SMMHC. RT-PCR[1] Cell Types: ME-1 and U937 cells Tested Concentrations: 1 μM Incubation Duration: 6, 12 hrs (hours) Experimental Results: Increased expression of RUNX3, CSF1R, and CEBPA. |
| Animal Protocol |
Animal/Disease Models: Mice (Cbfb+/MYH11:Ras+/G12D leukemic cells)[1]
Doses: 200 mg/kg Route of Administration: per day Experimental Results: decreased leukemia expansion in vivo and survived Dramatically long. |
| References |
[1]. Anuradha Illendula, et al. Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84.
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| Molecular Formula |
C30H22F6N6O5
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| Molecular Weight |
660.52
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| CAS # |
1256094-72-0
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| Related CAS # |
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| SMILES |
FC(OC1C([H])=C([H])C2=C(C=1[H])N([H])C(C1C([H])=C([H])C(=C([H])N=1)OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC1=C([H])N=C(C([H])=C1[H])C1=NC3C([H])=C([H])C(=C([H])C=3N1[H])OC(F)(F)F)=N2)(F)F
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO +90%PEG400: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5140 mL | 7.5698 mL | 15.1396 mL | |
| 5 mM | 0.3028 mL | 1.5140 mL | 3.0279 mL | |
| 10 mM | 0.1514 mL | 0.7570 mL | 1.5140 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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