10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site ofwild type and V600E mutant BRAFwith IC50 values of 79 nM and 38 nM, respectively. It also inhibitsCRAF, p38 and CSF1Rat sub 100 nM potencies.
Targets
p38 (Cell-free assay); CSF1R (Cell-free assay); BRAF(V600E) (Cell-free assay); CRAF (Cell-free assay); WT BRAF (Cell-free assay) 6 nM; 35 nM; 38 nM; 68 nM; 79 nM
In vitro
AZ304 shows potent inhibitory activities to the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 values of 79\u2009nM, 38\u2009nM and 68\u2009nM, respectively. AZ304 potently reduces ERK phosphorylation (p-ERK), with a mean EC50 of 65\u2009nM in the V600E mutant BRAF containing melanoma cell line A375 and an EC50 of 60\u2009nM 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\u2009μM in mutant BRAF cell lines, 0.43-11.7\u2009μM in wild type BRAF/RAS cell lines, and 0.9-16.66\u2009μM 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.
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.
Cell Research(from reference)
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
| ALogP | 5.524 |
|---|---|
| hba_count | 4 |
| Recuento HBD | 2 |
| Enlace rotable | 6 |
| Sonrisas canónicas | CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(C)(C)C#N)NC3=NC=NC4=C3C=CC(=C4)OC |
|---|---|
| IUPAC Name | 3-(2-cyanopropan-2-yl)-N-[3-[(7-methoxyquinazolin-4-yl)amino]-4-methylphenyl]benzamide |
| InChIKey | NGWQZRWVYYFTHC-UHFFFAOYSA-N |
| INCHI | 1S/C27H25N5O2/c1-17-8-9-20(31-26(33)18-6-5-7-19(12-18)27(2,3)15-28)13-23(17)32-25-22-11-10-21(34-4)14-24(22)29-16-30-25/h5-14,16H,1-4H3,(H,31,33)(H,29,30,32) |
| Isómeros 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 |
| Peso molecular | 451.52 |
| Reaxy-Rn | 12922408 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12922408&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Clase | Benzene and substituted derivatives |
| Subclass | Anilides |
| Intermediate Tree Nodes | Aromatic anilides |
| Direct Parent | Benzanilides |
| Alternative Parents | Quinazolinamines Phenylpropanes Benzamides Diaminotoluenes Aniline and substituted anilines Anisoles Benzoyl derivatives Alkyl aryl ethers Aminopyrimidines and derivatives Imidolactams Heteroaromatic compounds Amino acids and derivatives Secondary carboxylic acid amides Azacyclic compounds Nitriles Secondary amines Hydrocarbon derivatives Organic oxides |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Benzanilide - Quinazolinamine - Quinazoline - Benzamide - Benzoic acid or derivatives - Diaminotoluene - Phenylpropane - Anisole - Benzoyl - Phenol ether - Aniline or substituted anilines - Alkyl aryl ether - Aminopyrimidine - Toluene - Pyrimidine - Imidolactam - Heteroaromatic compound - Secondary carboxylic acid amide - Amino acid or derivatives - Carboxamide group - Secondary amine - Organoheterocyclic compound - Azacycle - Nitrile - Carbonitrile - Ether - Carboxylic acid derivative - Amine - Organonitrogen compound - Hydrocarbon derivative - Organic oxide - Cyanide - Organic oxygen compound - Organooxygen compound - Organic nitrogen compound - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene. |
| External Descriptors | Not available |
| DMSO (mg/ml) Solubilidad máxima | 90 |
|---|---|
| DMSO (mM) Solubilidad máxima | 199.326718639263 |
| Agua (mg/ml) Solubilidad máxima | ＜1 |
| Peso molecular | 451.500 g/mol |
| XLogP3 | 5.200 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 6 |
| Exact Mass | 451.201 Da |
| Monoisotopic Mass | 451.201 Da |
| Topological Polar Surface Area | 99.900 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 749.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
