2. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. IRAK FLT3
  4. IRAK1/4/pan-FLT3 Kinase-IN-1

IRAK1/4/pan-FLT3 Kinase-IN-1 is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 can be used for research on AML.

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

IRAK1/4/pan-FLT3 Kinase-IN-1

IRAK1/4/pan-FLT3 Kinase-IN-1 Chemical Structure

CAS No. : 2760328-82-1

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Other Forms of IRAK1/4/pan-FLT3 Kinase-IN-1:

IRAK1/4/pan-FLT3 Kinase-IN-1 Related Antibodies

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IRAK1 IRAK3 IRAK4

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  • Purity & Documentation

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Description

IRAK1/4/pan-FLT3 Kinase-IN-1 is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 can be used for research on AML[1].

IC50 & Target

IRAK1

5 nM (IC50)

IRAK4

0.6 nM (IC50)

IRAK1

0.53 nM (Kd)

IRAK4

0.096 nM (Kd)

In Vitro

IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) exhibits Kds of 0.53 nM, 0.096 nM and 0.074 nM against IRAK1, IRAK4 and FLT3, respectively[1].
IRAK1/4/pan-FLT3 Kinase-IN-1 exhibits IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively[1].
IRAK1/4/pan-FLT3 Kinase-IN-1 inhibits phosphorylation of FLT3 or IRAK substrates in MOLM14 (D835Y) or THP1 cells[1].

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

IRAK1/4/pan-FLT3 Kinase-IN-1 Related Antibodies
In Vivo

IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) (10 mg/kg; i.p.; 5th a week) produces significant prolongation of survival relative to vehicle in a mouse xenograft model of AML[1].

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

Animal Model: NSG-SGM3 mice were intravenously xenografted with MOLM14 AML tumor cells containing FLT3 (ITD) and (D835Y) mutations to form a xenograft model of AML[1].
Dosage: 10 mg/kg
Administration: i.p.; 5th a week
Result: Prolonged mice life span to a median of 33 days.
Molecular Weight

399.46

Formula

C21H26FN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(O)(C1=CN2C(C=C1OC)=NC=C2C3=NC(N[C@H]4CNCC[C@@H]4F)=CC=C3)C
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 : 5 mg/mL (12.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5034 mL 12.5169 mL 25.0338 mL
5 mM 0.5007 mL 2.5034 mL 5.0068 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 0.5 mg/mL (1.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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
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, 6 months; -20°C, 1 month. 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 2.5034 mL 12.5169 mL 25.0338 mL 62.5845 mL
5 mM 0.5007 mL 2.5034 mL 5.0068 mL 12.5169 mL
10 mM 0.2503 mL 1.2517 mL 2.5034 mL 6.2584 mL
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IRAK1/4/pan-FLT3 Kinase-IN-1 Related Classifications

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.

Keywords:

IRAK1/4/pan-FLT3 Kinase-IN-12760328-82-1IRAKFLT3Interleukin-1 receptor associated kinaseIL-1R associated kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3IRAK/pan-FLT3 kinase inhibitorIRAK1IRAK4AMLInhibitorinhibitorinhibit

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