1. MAPK/ERK Pathway
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  3. AZ 628

AZ 628 

Cat. No.: HY-11004 Purity: 99.56%
Handling Instructions

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.

For research use only. We do not sell to patients.

AZ 628 Chemical Structure

AZ 628 Chemical Structure

CAS No. : 878739-06-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
25 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

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-RafV600E

34 nM (IC50)

B-Raf

105 nM (IC50)

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-RASG13D. Inhibition of RAF with AZ 628 suppresses MEK and ERK phosphorylation. AZ 628 selectively affects viability in K-RAS mutant cells[2].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (110.74 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 2.

    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

*All of the co-solvents are provided by MCE.
References
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-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

451.52

Formula

C₂₇H₂₅N₅O₂

CAS No.

878739-06-1

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

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
AZ 628
Cat. No.:
HY-11004
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AZ 628

Cat. No.: HY-11004