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AZ628

Cat. No. M2319
AZ628 Structure
Size Price Availability Quantity
10mg USD 160 In stock
25mg USD 340 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AZ628 is a potent tyrosine protein inhibitor for wild-type CRAF and BRAF V600E with IC50 of 29 and 34 nM, respectively. AZ628 inhibits activities of preactivated wild-type B-Raf with an IC50 of 105, respectively. AZ628 also suppreses activities of a number of tyrosine protein kinases such as VEGFR2, DDR2, Lyn and Flt1. AZ628 also prevents anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and triggers apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. AZ628 is antiangiogenic based on inhibition of VEGFR2.

Protocol
Cell Experiment
Cell lines The human melanoma cell
Preparation method Cells were maintained at 37°C in a humidified atmposphere at 5% CO2 grown in RPMI 1640 supplemented with 10% FBS, 100 IU/mL penicillin, 100 μg/mL streptomycin and 2nM glutamine. AZ628 resistant M14 clones were maintained in the above-mentioned medium and 2 μM of AZ628, except where otherwise indicated. The BRAF inhibitor AZ628 was synthesized by Astra Zeneca.
Concentrations 2 μM
Incubation time 16 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 451.52
Formula C27H25N5O2
CAS Number 878739-06-1
Purity >98%
Solubility DMSO 70 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Cancer Discov (2013). Figure 5. AZ628
Method Western blotting
Cell Lines A375 cells
Concentrations 0.2 μM
Incubation Time 16 h
Results In contrast to the aforementioned drug conditions, only minimal resistance (2-fold) was observed to AZ628
Rating
References

A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition.
Whittaker SR, et al. Cancer Discov. 2013 Mar;3(3):350-62. PMID: 23288408.

Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma.
Montagut C, et al. Cancer Res. 2008 Jun 15;68(12):4853-61. PMID: 18559533.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZ628 supplier, Raf, inhibitors

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