WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408020
Description: AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF. AZ304 exerts anti-tumour effects in colorectal cancer independently of BRAF genetic status. AZ304 exerted potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF, with IC50 values of 79 nM and 38 nM, respectively.
MedKoo Cat#: 408020
Chemical Formula: C27H25N5O2
Exact Mass: 451.2008
Molecular Weight: 451.53
Elemental Analysis: C, 71.82; H, 5.58; N, 15.51; O, 7.09
Synonym: AZ304; AZ-304; AZ 304;
IUPAC/Chemical Name: 3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide
InChi Key: NGWQZRWVYYFTHC-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NC1=CC=C(C)C(NC2=C3C=CC(OC)=CC3=NC=N2)=C1)C4=CC=CC(C(C)(C#N)C)=C4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 451.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Ma R, Xu L, Qu X, Che X, Zhang Y, Fan Y, Li C, Guo T, Hou K, Hu X, Drew L,
Shen M, Cheung T, Liu Y. AZ304, a novel dual BRAF inhibitor, exerts anti-tumour
effects in colorectal cancer independently of BRAF genetic status. Br J Cancer.
2018 May;118(11):1453-1463. doi: 10.1038/s41416-018-0086-x. Epub 2018 May 14.
PubMed PMID: 29755114; PubMed Central PMCID: PMC5988692.
By suppressing ERK phosphorylation, AZ304 effectively inhibited a panel of human cancer cell lines with different BRAF and RAS genetic statuses. In selected colorectal cancer cell lines, AZ304 significantly inhibited cell growth in vitro and in vivo, regardless of BRAF genetic status. In addition, the EGFR inhibitor Cetuximab enhanced the potency of AZ304 independently of BRAF mutational status.