2. Immunology/Inflammation
  3. IRAK
  4. AZ1495

AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

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

AZ1495 Chemical Structure

AZ1495 Chemical Structure

CAS No. : 2196204-23-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 380 In-stock
Solution
10 mM * 1 mL in DMSO USD 380 In-stock
Solid
1 mg USD 185 In-stock
5 mg USD 340 In-stock
10 mg USD 550 In-stock
25 mg USD 780 In-stock
50 mg USD 1100 In-stock
100 mg USD 1700 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

AZ1495 Related Antibodies

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IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL)[1].

IC50 & Target[1]

IRAK4

5 nM (IC50)

IRAK1

23 nM (IC50)

CLK1

50 nM (IC50)

CLK2

5 nM (IC50)

CLK4

8 nM (IC50)

haspin

4 nM (IC50)

In Vitro

AZ1495 (compound 28) (10 μM,1 h) has kinase selectivity for IRAK4 with IC50 values of 0.005 μM (enzyme assay) and 0.052 μM (cellular assay), respectively[1].
AZ1495 (10 μM,1 h) has kinase inhibition for IRAK4 with an IC50 value of 0.005 μM and Kd value of 0.0007 μM[1].
AZ1495 (0.001-100 μM, 72 h) inhibits NF-κB activation and growth of ABC-DLBCL cell lines in a dosedependent manner[1].
AZ1495 (0-3.3 μM, 14 h) completely inhibits NF-κB signaling and induces cell death at lower concentration in combination with a BTK inhibitor in OCI-LY10 cells[1].

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

AZ1495 Related Antibodies

Cell Viability Assay[1]

Cell Line: OCI-LY10 and SUDHL2 cells
Concentration: 0.001-100 μM
Incubation Time: 72 h
Result: Inhibited growth of OCI-LY10 cells in a dosedependent manner, whereas SUDHL2, a GCB-cell line was not sensitive and no increased cell killing to IRAK4 inhibitor.
Increased the cell death in OCI-LY10 cells upon increasing concentrations of compound 28 and BTK ibrutinib.

Western Blot Analysis[1]

Cell Line: OCI-LY10 cells
Concentration: 0-3.3 μM
Incubation Time: 14 h
Result: Inhibited IκBα phosphorylation with dose-dependentence in OCI-LY10 cells.
Showed induction of apoptosis combination with 10 nM ibrutinib by cleavage of caspase 3 in OCI-LY10 cells.
In Vivo

AZ1495 (compound 28) (oral, daily, 12.5 mg/kg) leds to tumor regression combination with ibrutinib in an ABC-DLBCL mouse model (OCI-LY10 cells)[1].
AZ1495 (iv., 2 mg/kg and oral, 5mg/kg) is characterized by high clearance (Cl) in rat (75 mL/min/kg) and moderate predictions based on hepatocyte data (Clint 15 μl/min/106 cells, predicted clearance 42 mL/min/kg) with low bioavailability consistent with a high first pass effect[1].
AZ1495 (iv., 1 mg/kg) has low the amount of active renal secretion occurring in the dog[1].

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

Animal Model: CB.17 SCID mice[1]
Dosage: 12.5 mg/kg
Administration: oral, daily, 12.5 mg/kg
Result: Had modest anti-tumor activity as single agents but a combination ofibrutinib led to tumor regression and is well tolerated.
Animal Model: rat[1]
Dosage: 2 mg/kg, 5mg/kg
Administration: iv., 2 mg/kg and oral, 5mg/kg
Result:
Species Dose (mg/kg) Cl (mL/min/kg) Vss(L/kg) PO halflife (h) IV halflife (h) Fabs (%) F (%)
Rat 2，5 75 2.1 2.0 0.8 100 28
Dog 1 29 3.0 - 3.3 - -
Animal Model: dog[1]
Dosage: 1 mg/kg
Administration: iv., 1 mg/kg
Result:
Species Dose (mg/kg) Cl (mL/min/kg) Vss(L/kg) PO halflife (h) IV halflife (h) Fabs (%) F (%)
Rat 2，5 75 2.1 2.0 0.8 100 28
Dog 1 29 3.0 - 3.3 - -
Molecular Weight

385.50

Formula

C21H31N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(C(C2CCOCC2)=CN3)=C3N=CN=C1N[C@@H]4CC[C@@H](N5CCOCC5)CC4
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 : 10 mg/mL (25.94 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 2.5940 mL 12.9702 mL 25.9403 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 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

  • 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: ≥ 1 mg/mL (2.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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

Purity: 98.07%

COA (253 KB) RP-HPLC (257 KB)

Handling Instructions (2659 KB)
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 2.5940 mL 12.9702 mL 25.9403 mL 64.8508 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 mL 12.9702 mL
10 mM 0.2594 mL 1.2970 mL 2.5940 mL 6.4851 mL
15 mM 0.1729 mL 0.8647 mL 1.7294 mL 4.3234 mL
20 mM 0.1297 mL 0.6485 mL 1.2970 mL 3.2425 mL
25 mM 0.1038 mL 0.5188 mL 1.0376 mL 2.5940 mL
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AZ1495 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:

AZ14952196204-23-4AZ 1495AZ-1495IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseweak baseinterleukin-1 receptor associated kinase 4 (IRAK4)interleukin-1 receptor associated kinase 1 (IRAK1)diffuse large B-cell lymphoma (DLBCL)cancerInhibitorinhibitorinhibit

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