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AI-10-49 

Cat. No.: HY-16786 Purity: 99.24%
Handling Instructions

AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 348 In-stock
Estimated Time of Arrival: December 31
50 mg USD 588 In-stock
Estimated Time of Arrival: December 31
100 mg USD 792 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM. IC50 value: 0.26 uM [1] Target: CBFβ-SMMHC/RUNX1 interaction inhibitor AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that 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.

Molecular Weight

660.52

Formula

C₃₀H₂₂F₆N₆O₅

CAS No.

1256094-72-0

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (51.47 mM)

*"≥" 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
10 mM 0.1514 mL 0.7570 mL 1.5140 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.24%

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Keywords:

AI-10-49OthersInhibitorinhibitorinhibit

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