| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
AZ-628 (AZ628; AZ 628) is a novel, selective, and orally bioavailable Raf inhibitor with potential anticancer activity. In xenograft animal models, it demonstrates strong tumor growth inhibition and excellent pharmacokinetic characteristics. With respective IC50 values of 29, 34, and 105 nM, AZ-628 inhibits the Raf isoforms c-Raf1, B-RafV600E, and wild-type B-Raf. In colon and melanoma cell lines with the B-RafV600E mutation, AZ-628 potently inhibits the proliferation and causes cell cycle arrest and apoptosis.
| Targets |
c-Raf-1 (IC50 = 29 nM); B-Raf (V600E) (IC50 = 34 nM); B-Raf (IC50 = 105 nM)
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| ln Vitro |
AZ 628 reduces the activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34, and 29 nM, respectively. A number of other tyrosine protein kinases, such as VEGFR2, DDR2, Lyn, Flt1, and FMS, are also prevented from activating by AZ 628. In colon and melanoma cell lines carrying the B-RafV600E mutation, AZ 628 inhibits anchorage-dependent and -independent growth, results in cell cycle arrest, and induces apoptosis[1].
AZ 628 inhibits the growth of cells that are K-RASG13D-expressing. MEK and ERK phosphorylation is reduced when RAF is inhibited with AZ 628. Viability in K-RAS mutant cells is selectively impacted by AZ 628[2]. |
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| ln Vivo |
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| Enzyme Assay |
AZ 628 is a pan-Raf kinase inhibitor with IC50 values for B-Raf, B-RafV600E, and c-Raf-1 of 105, 34, and 29 nM, respectively.
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| Cell Assay |
In HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines, cell viability was measured by Syto60 after 72 hours of treatment with AZ 628 (0.5, 1.0, and 1.5 μM), CI-1040, or BAY61-3606. Each cell line's relative cell viability is normalized to the control that received DMSO treatment[2].
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| Animal Protocol |
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| References |
| Molecular Formula |
C27H25N5O2
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| Molecular Weight |
451.52
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| Exact Mass |
451.20
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| Elemental Analysis |
C, 71.82; H, 5.58; N, 15.51; O, 7.09
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| CAS # |
878739-06-1
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(C)(C)C#N)NC3=CC4=C(C=C3)N=CN(C4=O)C
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| InChi Key |
ZGBGPEDJXCYQPH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H25N5O2/c1-17-8-9-21(31-25(33)18-6-5-7-19(12-18)27(2,3)15-28)14-24(17)30-20-10-11-23-22(13-20)26(34)32(4)16-29-23/h5-14,16,30H,1-4H3,(H,31,33)
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| Chemical Name |
3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide
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| Synonyms |
AZ-628; AZ 628; AZ628
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 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 25.0 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: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL |
| 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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