AZ 628
Based on 12 publication(s) in Google Scholar
AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.44%
- No. CAS: 878739-06-1
- Fòrmula: C27H25N5O2
- Peso molecular:451.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AZ 628
More- Cell Stem Cell. 2025 Oct 2;32(10):1509-1527.e9. [Abstract]
- Exp Mol Med. 2021 Apr;53(4):572-590. [Abstract]
- Cell Discov. 2023 Mar 7;9(1):26. [Abstract]
- Nat Chem Biol. 2026 May 12:10.1038/s41589-026-02212-2. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Mol Syst Biol. 2015 Mar 26;11(3):797. [Abstract]
- Int Immunopharmacol. 2022 Oct:111:109085. [Abstract]
- Genes (Basel). 2022 Nov 2;13(11):2011. [Abstract]
- J Chem Eng Data. 2024 Jun 10.
- bioRxiv. 2024 August 16.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- bioRxiv. 2019 Sep.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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IF
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Histological Imaging/Staining
Actividad biológica
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c-Raf-1 29 nM (IC50) |
B-RafV600E 34 nM (IC50) |
B-Raf 105 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A-375 | IC50 |
0.04 μM
Compound: 3; AZ628
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Cytotoxicity against human A-375 cells incubated for 96 hrs by MTT assay
Cytotoxicity against human A-375 cells incubated for 96 hrs by MTT assay
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[PMID: 36878151] |
| A-375 | IC50 |
15 nM
Compound: 2, AZ628
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Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins
Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins
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[PMID: 23398453] |
| M14 | IC50 |
0.1 μM
Compound: 125; AZ628
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Antiproliferative activity against human M14 cells
Antiproliferative activity against human M14 cells
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[PMID: 32798788] |
| Malme-3M | IC50 |
27 nM
Compound: AZ-268
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Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation
Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation
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[PMID: 24675381] |
| Melanoma cell line | IC50 |
10 μM
Compound: 125; AZ628
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Antiproliferative activity against human Melanoma cell line
Antiproliferative activity against human Melanoma cell line
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[PMID: 32798788] |
| Sf9 | IC50 |
0.27 μM
Compound: 2, AZ628
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Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP
Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP
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[PMID: 23398453] |
| Sf9 | IC50 |
2.64 μM
Compound: 2, AZ628
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Inhibition of human recombinant N-terminus His-tagged BRAF expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP
Inhibition of human recombinant N-terminus His-tagged BRAF expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP
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[PMID: 23398453] |
| Sf9 | IC50 |
34 nM
Compound: 2, AZ628
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Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 10 uM ATP
Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 10 uM ATP
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[PMID: 23398453] |
| SW-620 | IC50 |
0.17 μM
Compound: 3; AZ628
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Cytotoxicity against human SW620 cells incubated for 96 hrs by MTT assay
Cytotoxicity against human SW620 cells incubated for 96 hrs by MTT assay
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[PMID: 36878151] |
AZ 628 reduces 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. AZ 628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ 628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation[1].
AZ 628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ 628 suppresses MEK and ERK phosphorylation. AZ 628 selectively affects viability in K-RAS mutant cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 878739-06-1
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Appearance Solid
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Peso molecular 451.52
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Fòrmula C27H25N5O2
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Color Off-white to pink
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SMILES
O=C1N(C)C=NC2=C1C=C(C=C2)NC3=C(C)C=CC(NC(C4=CC(C(C#N)(C)C)=CC=C4)=O)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Exp Mol Med
Sublytic C5b-9 induces glomerular mesangial cell proliferation via ERK1/2-dependent SOX9 phosphorylation and acetylation by enhancing Cyclin D1 in rat Thy-1 nephritis. [Abstract]2021 Apr;53(4):572-590. PMID: 33811247 -
Cell Discov
Reprogramming of palmitic acid induced by dephosphorylation of ACOX1 promotes β-catenin palmitoylation to drive colorectal cancer progression. [Abstract]2023 Mar 7;9(1):26. PMID: 36878899 -
Nat Chem Biol
2026 May 12:10.1038/s41589-026-02212-2. PMID: 42120500 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
Mol Syst Biol
Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. [Abstract]2015 Mar 26;11(3):797. PMID: 25814555 -
Int Immunopharmacol
AZ-628 delays osteoarthritis progression via inhibiting the TNF-α-induced chondrocyte necroptosis and regulating osteoclast formation. [Abstract]2022 Oct:111:109085. PMID: 35952515
AZ 628 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Oct:111:109085. [Abstract]
The CCK-8 assay was used to determine the toxicity of AZ-628 (1.25, 2.5, 5, 10, 20, 40, 80, 160, 320 nM) to ATDC5 at 24, 48, and 72 h.
AZ 628 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Oct:111:109085. [Abstract]
The NF-κB signaling pathway proteins of ATDC5 including IKKα/β, IκBα, P65, and their phosphorylated proteins were detected by Western blot. Cells were pretreated with different combinations of TNF-α (10 ng/mL) and AZ-628 (1.25, 2.5, 5 nM) for 48 h.
AZ 628 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Oct:111:109085. [Abstract]
The P65 was detected by immunofluorescence combined with DAPI staining for nuclei treated with AZ-628 (1.25, 2.5, 5 nM).
AZ 628 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Oct:111:109085. [Abstract]
Histological staining analysis of the visceral tissues treated with AZ 628 (15, 30 mg/kg, i.p.).
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Genes (Basel)
Integrative Transcriptomic Analysis Identify Potential m6A Pathway-Related Drugs That Inhibit Cancer Cell Proliferation. [Abstract]2022 Nov 2;13(11):2011. PMID: 36360248 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (110.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell viability quantified by Syto60 after 72 hours of AZ 628 (0.5, 1.0, and 1.5 μM), CI-1040 or BAY61-3606 treatment in HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | 55.3685 mL |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | 11.0737 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL | 5.5369 mL | |
| 15 mM | 0.1476 mL | 0.7382 mL | 1.4765 mL | 3.6912 mL | |
| 20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7684 mL | |
| 25 mM | 0.0886 mL | 0.4429 mL | 0.8859 mL | 2.2147 mL | |
| 30 mM | 0.0738 mL | 0.3691 mL | 0.7382 mL | 1.8456 mL | |
| 40 mM | 0.0554 mL | 0.2768 mL | 0.5537 mL | 1.3842 mL | |
| 50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1074 mL | |
| 60 mM | 0.0369 mL | 0.1846 mL | 0.3691 mL | 0.9228 mL | |
| 80 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6921 mL | |
| 100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 mL |
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