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AZD9291

Cat. No. M2424
AZD9291 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 70 In stock
10mg USD 100 In stock
50mg USD 180 In stock
100mg USD 260 In stock
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Quality Control
Biological Activity

AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. In vivo, AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines when compared with wild-type. AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK .

Protocol
Cell Experiment
Cell lines PC-9, H1975, LOVO, H1650 and H3255 lines
Preparation method In vitro EGFR phosphorylation assays Cells were treated for 2 h with a dose-response of each drug. Wild-type cells were stimulated for 10 minutes with 25 ng/ml of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using a modified R&D Systems DuoSet Human phospho-EGFR ELISA (36).
Concentrations 0-1000nM
Incubation time 2h
Animal Experiment
Animal models PC-9 and H1975 cells subcutaneous xenograft models
Formulation not mentioned
Dosages 5 mg/kg/day QD
Administration oral
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 499.61
Formula C28H33N7O2
CAS Number 1421373-65-0
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Nat Med (2015). Figure 1. AZD9291
Method digital PCR (ddPCR) assay
Cell Lines Ba/F3 cells
Concentrations 1.0 μM
Incubation Time 72 h
Results Although a more comprehensive analysis of plasma and biopsy tissue collected after resistance develops will be needed to provide greater clarity on C797S mutation incidence, the emergence of this mutation in a marked proportion of AZD9291-resistant patients suggests that development of targeted therapies with the ability to overcome the C797S mutation is warranted.
Rating
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD9291 supplier, EGFR/HER2, inhibitors

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