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AI-10-49 is an inhibitor of leukemic oncoprotein CBFβ-SMHHC. AI-10-49 inhibits the binding of CBFβ-SMMHCto the RUNX1 Runt domain with IC50 value of 0.26 μM. AI-10-49 can be used for the research of leukemia.

For research use only. We do not sell to patients.

AI-10-49 Chemical Structure

AI-10-49 Chemical Structure

CAS No. : 1256094-72-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 166 In-stock
Solution
10 mM * 1 mL in DMSO USD 166 In-stock
Solid
5 mg USD 114 In-stock
10 mg USD 180 In-stock
25 mg USD 348 In-stock
50 mg USD 588 In-stock
100 mg USD 792 In-stock
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Description

AI-10-49 is an inhibitor of leukemic oncoprotein CBFβ-SMHHC. AI-10-49 inhibits the binding of CBFβ-SMMHCto the RUNX1 Runt domain with IC50 value of 0.26 μM. AI-10-49 can be used for the research of leukemia[1].

Cellular Effect
Cell Line Type Value Description References
Caco-2 IC50
0.19 μM
Compound: AI-10-49
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
Caco-2 CC50
6.58 μM
Compound: AI-10-49
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
In Vitro

AI-10-49 inhibits the binding of CBFβ-SMMHCto theRUNX1 Runt domain with IC50 value of 0.26 μM[1].
? AI-10-49 (1 μM; 3, 6, 12 hours) has selectivity for inhibiting CBFβ-SMMHC binding to RUNX1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: ME-1 cells
Concentration: 1 μM
Incubation Time: 3, 6 hours
Result: Effectively dissociated RUNX1 from CBFβ-SMMHC.

RT-PCR[1]

Cell Line: ME-1 and U937 cells
Concentration: 1 μM
Incubation Time: 6, 12 hours
Result: Increased expression of RUNX3, CSF1R, and CEBPA.
In Vivo

AI-10-49 (200 mg/kg; per day) delays leukemia progression in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice (Cbfb+/MYH11:Ras+/G12D leukemic cells)[1]
Dosage: 200 mg/kg
Administration: per day
Result: Reduced leukemia expansion in vivo and survived significantly long.
Molecular Weight

660.52

Formula

C30H22F6N6O5

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

FC(F)(F)OC1=CC=C2N=C(C3=NC=C(OCCOCCOC4=CN=C(C5=NC6=CC=C(OC(F)(F)F)C=C6N5)C=C4)C=C3)NC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (51.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.24%

References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5140 mL 7.5698 mL 15.1396 mL 37.8490 mL
5 mM 0.3028 mL 1.5140 mL 3.0279 mL 7.5698 mL
10 mM 0.1514 mL 0.7570 mL 1.5140 mL 3.7849 mL
15 mM 0.1009 mL 0.5047 mL 1.0093 mL 2.5233 mL
20 mM 0.0757 mL 0.3785 mL 0.7570 mL 1.8924 mL
25 mM 0.0606 mL 0.3028 mL 0.6056 mL 1.5140 mL
30 mM 0.0505 mL 0.2523 mL 0.5047 mL 1.2616 mL
40 mM 0.0378 mL 0.1892 mL 0.3785 mL 0.9462 mL
50 mM 0.0303 mL 0.1514 mL 0.3028 mL 0.7570 mL
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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.

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AI-10-49
Cat. No.:
HY-16786
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