Home MAPK Raf inhibitor AZ304 For research use only.

AZ304

AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100 nM potencies.

AZ304 Chemical Structure

AZ304 Chemical Structure

CAS: 942507-42-8

Purity & Quality Control

Batch: S875501 DMSO] 90 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

Other Raf Products

Related compound libraries

Choose Selective Raf Inhibitors

Biological Activity

Description AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100 nM potencies.
Targets
p38 [1]
(Cell-free assay)		 CSF1R [1]
(Cell-free assay)		 BRAF(V600E) [1]
(Cell-free assay)		 CRAF [1]
(Cell-free assay)		 WT BRAF [1]
(Cell-free assay)
6 nM 35 nM 38 nM 68 nM 79 nM
In vitro
In vitro

AZ304 shows potent inhibitory activities to the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF in vitro, with IC50 values of 79 nM, 38 nM and 68 nM, respectively. AZ304 potently reduces ERK phosphorylation (p-ERK), with a mean EC50 of 65 nM in the V600E mutant BRAF containing melanoma cell line A375 and an EC50 of 60 nM in the wild type BRAF containing melanoma cell line SK-MEL-31. AZ304 markedly inhibits cell proliferation in mutant BRAF cancer cell lines, and effectively reduces cell growth in selected cell lines harbouring wild type BRAF/RAS or mutant RAS. The GI50 values ranged from 0.08-7.72 μM in mutant BRAF cell lines, 0.43-11.7 μM in wild type BRAF/RAS cell lines, and 0.9-16.66 μM in mutant RAS cell lines. AZ304 exhibits anti-proliferative effects on multiple cancer types, including melanoma, colorectal cancer, leukaemia, ovarian cancer, lung cancer, and pancreatic cancer, independently of BRAF genetic status. AZ304 retains inhibitory activity against both V600E mutant and wild type BRAF CRC cell lines in the presence of the EGFR ligand EGF[1].
Cell Research Cell lines cell lines containing wild type BRAF or V600E mutant BRAF (MC-F7, A549 and A375 cells)
Concentrations 6.5 nM, 65 nM, 650 nM and 6.5 μM
Incubation Time 75 min
Method

In vitro p-ERK and p-P38 evaluation in cell lines containing wild type BRAF or V600E mutant BRAF: Cells are collected following 75 min treatment at 0.1, 1, 10 and 100 fold of A375 p-ERK EC50 for each compound. (A375: BRAF V600E, A549: RAS MT; MC-F7: BRAF/RAS WT)
In Vivo
In vivo

AZ304 monotherapy and its combination with Cetuximab have anti-tumour effects on RKO and Caco-2 tumour xenografts without obvious toxicity, independently of BRAF mutation status[1].
Animal Research Animal Models Female 4-6 weeks old athymic BALB/c nude mice inoculated with RKO/Caco-2 cells
Dosages 10 mg/kg
Administration by oral gavage

Chemical lnformation & Solubility

Molecular Weight 451.52 Formula

C27H25N5O2
CAS No. 942507-42-8 SDF --
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(C)(C)C#N)NC3=NC=NC4=C3C=CC(=C4)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (199.32 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy AZ304|AZ304 ic50|AZ304 price|AZ304 cost|AZ304 solubility dmso|AZ304 purchase|AZ304 manufacturer|AZ304 research buy|AZ304 order|AZ304 mouse|AZ304 chemical structure|AZ304 mw|AZ304 molecular weight|AZ304 datasheet|AZ304 supplier|AZ304 in vitro|AZ304 cell line|AZ304 concentration|AZ304 nmr|AZ304 in vivo|AZ304 clinical trial|AZ304 inhibitor|AZ304 MAPK inhibitor