Home MAPK Raf inhibitor AZ304

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AZ304 Raf inhibitor

Cat.No.S8755

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 Raf inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 451.52

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 451.52 Formula

C27H25N5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 942507-42-8 -- Storage of Stock Solutions

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
p38
(Cell-free assay)
6 nM
CSF1R
(Cell-free assay)
35 nM
BRAF(V600E)
(Cell-free assay)
38 nM
CRAF
(Cell-free assay)
68 nM
WT BRAF
(Cell-free assay)
79 nM
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. This compound 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. It 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. This chemical 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. It retains inhibitory activity against both V600E mutant and wild type BRAF CRC cell lines in the presence of the EGFR ligand EGF.
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.
References

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