ChemicalBook--->CAS DataBase List--->942507-42-8

942507-42-8

942507-42-8 Structure

942507-42-8 Structure
IdentificationBack Directory
[Name]

AZ304
[CAS]

942507-42-8
[Synonyms]

AZ304
AZ304;AZ-304;AZ 304
3-(2-Cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide
3-(2-Cyano-2-propanyl)-N-{3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl}benzamide
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]-
[Molecular Formula]

C27H25N5O2
[MOL File]

942507-42-8.mol
[Molecular Weight]

451.52
Chemical PropertiesBack Directory
[Boiling point ]

582.6±50.0 °C(Predicted)
[density ]

1.270±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[pka]

12.87±0.70(Predicted)
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
[HS Code ]

2933998090
Hazard InformationBack Directory
[Uses]

AZ304 is potent dual BRAF inhibitor. Is a combination of MEK and B-raf inhibitors for treatment of cancer.
[Biological Activity]

AZ304 is a synthetic inhibitor targeting wild-type and V600E mutant BRAF with IC50 of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R with IC50 below 100 nM.
[in vitro]

AZ304 inhibited wild-type BRAF and CRAF, BRAF in vitro.

[in vivo]

In both RKO and Caco-2 tumor models, administration of AZ304 alone or in combination with Cetuximab resulted in antitumor activity without apparent toxic effects (regardless of BRAF mutation).

[target]

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BRAF(V600E)
(Cell-free assay) < /tr>
TargetValue
p38
(Cell-free assay)
6 nM
CSF1R
(Cell-free assay)
35 nM
38 nM
CRAF
(Cell-free assay )
68 nM
WT BRAF
(Cell-free assay)
79 nM
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