Art. -Nr.: HY-11004

AZ 628

12 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.44%
CAS. Nr.: 878739-06-1
Formel: C₂₇H₂₅N₅O₂
Molecular Weight:451.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AZ 628 Chemical Structure

CAS. Nr.: 878739-06-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target^[1]

c-Raf-1

29 nM (IC₅₀)

B-Raf^V600E

34 nM (IC₅₀)

B-Raf

105 nM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.04 μM Compound: 3; AZ628	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	[PMID: 36878151]
A-375	IC₅₀	15 nM Compound: 2, AZ628	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	[PMID: 23398453]
M14	IC₅₀	0.1 μM Compound: 125; AZ628	Antiproliferative activity against human M14 cells Antiproliferative activity against human M14 cells	[PMID: 32798788]
Malme-3M	IC₅₀	27 nM Compound: AZ-268	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	[PMID: 24675381]
Melanoma cell line	IC₅₀	10 μM Compound: 125; AZ628	Antiproliferative activity against human Melanoma cell line Antiproliferative activity against human Melanoma cell line	[PMID: 32798788]
Sf9	IC₅₀	0.27 μM Compound: 2, AZ628	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	[PMID: 23398453]
Sf9	IC₅₀	2.64 μM Compound: 2, AZ628	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	[PMID: 23398453]
Sf9	IC₅₀	34 nM Compound: 2, AZ628	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	[PMID: 23398453]
SW-620	IC₅₀	0.17 μM Compound: 3; AZ628	Cytotoxicity against human SW620 cells incubated for 96 hrs by MTT assay Cytotoxicity against human SW620 cells incubated for 96 hrs by MTT assay	[PMID: 36878151]

In Vitro

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-RAS^G13D. 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

CAS. Nr. 878739-06-1
Appearance Solid
Molecular Weight 451.52
Formel C₂₇H₂₅N₅O₂
Color Off-white to pink
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All Cell Proliferation/Viability AssayWBIFHistological Imaging/Staining

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Journal Impact Factor

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

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition. [Abstract]

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.).
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
J Chem Eng Data

2024 Jun 10.
bioRxiv

2024 August 16.
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
bioRxiv

2019 Sep.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[2]

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-RAS^G13D/+) 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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Khazak V, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609. [Content Brief]

[2]. Lau KS, et al. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AZ 628

12 Cited Publications

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AZ 628

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Publications Citing Use of MedChemExpress (MCE) AZ 628

Alle Raf Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ 628

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Publications Citing Use of MedChemExpress (MCE) AZ 628

Alle Raf Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ 628 Related Classifications

HY-11004 Related Classifications