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AZD-9291 (Mesylate)

Cat. No. M5099
AZD-9291 (Mesylate) Structure
Synonym:

Mereletinib Mesylate

Size Price Availability Quantity
5mg USD 55 In stock
10mg USD 80 In stock
50mg USD 140 In stock
100mg USD 200 In stock
200mg USD 320 In stock
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Quality Control
Biological Activity

AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.12.92 nM(Exon 19 deletion EGFR); 11.44 nM(L858R/T790M EGFR)

Protocol
Cell Experiment
Cell lines PC-9 cells
Preparation method Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved.
Concentrations 160 nM
Incubation time 48 h
Animal Experiment
Animal models Mice
Formulation 1% Polysorbate 80
Dosages 7.5 mg/kg and 5 mg/kg
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 595.71
Formula C29H37N7O5S
CAS Number 1421373-66-1
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67. PMID: 25271963.

AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
Cross DA, et al. Cancer Discov. 2014 Sep;4(9):1046-61. PMID: 24893891.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD-9291 (Mesylate), Mereletinib Mesylate supplier, EGFR/HER2, inhibitors

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