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

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

Cat. No.: HY-159953A Purity: 98.46%
Handling Instructions Technical Support

IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride 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 hydrochloride can be used for research on AML.

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

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

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

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Description

IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride 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 hydrochloride can be used for research on AML[1].

IC50 & Target[1]

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) hydrochloride 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 hydrochloride 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 hydrochloride 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.

Parmacokinetics
Species Dose Route CLplasma T1/2 F AUC
Dog[1] 1/3 mg/kg i.v. 0.3 mL/min/kg 12.2 h / /
Dog[1] 1/3 mg/kg p.o. / / 100 % 237.5 μM·h
Mice[1] 1/3 mg/kg i.v. 120 mL/min/kg 2.4 h / /
Mice[1] 1/3 mg/kg p.o. / / 25 % 1.39 μM·h
Rat[1] 1/3 mg/kg i.v. 3 mL/min/kg 4.0 h / /
Rat[1] 1/3 mg/kg p.o. / / 60 % 31.8 μM·h
In Vivo

IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) (10 mg/kg; i.p.; 5th a week) hydrochloride 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

435.92

Formula

C21H27ClFN5O2

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.Cl

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 : 200 mg/mL (458.80 mM; Need ultrasonic; 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 2.2940 mL 11.4700 mL 22.9400 mL
5 mM 0.4588 mL 2.2940 mL 4.5880 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

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 2.2940 mL 11.4700 mL 22.9400 mL 57.3500 mL
5 mM 0.4588 mL 2.2940 mL 4.5880 mL 11.4700 mL
10 mM 0.2294 mL 1.1470 mL 2.2940 mL 5.7350 mL
15 mM 0.1529 mL 0.7647 mL 1.5293 mL 3.8233 mL
20 mM 0.1147 mL 0.5735 mL 1.1470 mL 2.8675 mL
25 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2940 mL
30 mM 0.0765 mL 0.3823 mL 0.7647 mL 1.9117 mL
40 mM 0.0573 mL 0.2867 mL 0.5735 mL 1.4337 mL
50 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1470 mL
60 mM 0.0382 mL 0.1912 mL 0.3823 mL 0.9558 mL
80 mM 0.0287 mL 0.1434 mL 0.2867 mL 0.7169 mL
100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.5735 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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Product Name:
IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride
Cat. No.:
HY-159953A
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