| Identification | Back 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 Properties | Back 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 | [form ]
Solid | [pka]
12.87±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back 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]
| Target | Value | p38
(Cell-free assay) | 6 nM | CSF1R
(Cell-free assay) | 35 nM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BRAF(V600E)
(Cell-free assay) 38 nM | CRAF
(Cell-free assay ) | 68 nM | WT BRAF
(Cell-free assay) | 79 nM | < /tr>
| [IC 50]
BRafV600E: 38 nM (IC50); BRAFWT: 79 nM (IC50); CRAF: 68 nM (IC50); p38: 6 nM (IC50); CSF1R: 35 nM (IC50); MAP3K7: 6400 nM (IC50); CSK: 7050 nM (IC50) |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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