| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
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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|---|---|
| ln Vitro |
AZ304 (1 nM–100 μM) significantly lowers p-ERK phosphorylation; in the V600E mutant BRAF-containing melanoma cell line A375, the mean EC50 was 65 nM, whereas in the wild type BRAF melanoma cell line SK-MEL-31, both with and without EGF, the EC50s were 52 nM and 60 nM[1]. In both BRAF genetic status cell lines, AZ304 also strongly suppresses p-p38[1]. With GI50s of 4.539 μM, 3.896 μM, 4.987 μM, 1.763 μM (48 hours) and 0.5032 μM, 0.3887 μM, 0.6354 μM, 0.3772 μM (72 hours), respectively, AZ304 (0, 0.1, 1, 10, 100 μM, 48 and 72 hours) dose-dependently suppresses the growth of RKO, HT-29, DiFi, and Caco-2[1]. AZ304 (2 μM, 36 and 48 hours) raises p-EGFR in BRAF wild type and BRAF V600E mutant cells while decreasing BRAF, p-ERK, p-AKT, and p-mTOR levels. When combined with C225, AZ304 more effectively reduces the BRAF, ERK, AKT, and mTOR signaling pathways while downregulating p-EGFR and inhibiting p-ERK[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: RKO, HT-29, DiFi, Caco-2 cells Tested Concentrations: 0, 0.1, 1, 10, 100 μM Incubation Duration: 48, 72 hrs (hours) Experimental Results: Dose- dependently inhibited the growth of V600E mutant BRAF cell lines (RKO, HT-29) and wild-type BRAF cell lines (DiFi, Caco-2). |
| References |
[1]. Ma R, et al. 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.
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| Molecular Formula |
C27H25N5O2
|
|---|---|
| Molecular Weight |
451.52
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| Exact Mass |
451.2
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| Elemental Analysis |
C, 71.82; H, 5.58; N, 15.51; O, 7.09
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| CAS # |
942507-42-8
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| SMILES |
O=C(NC1=CC=C(C)C(NC2=C3C=CC(OC)=CC3=NC=N2)=C1)C4=CC=CC(C(C)(C#N)C)=C4
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| InChi Key |
NGWQZRWVYYFTHC-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide
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| Synonyms |
AZ304; AZ-304; AZ 304;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (276.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.61 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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