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Osimertinib

Osimertinib
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Purity:100%
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Osimertinib

Catalog No. T2490Cas No. 1421373-65-0
Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
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Pack SizePriceAvailabilityQuantity
2 mg$25.6$32In Stock
5 mg$38.4$48In Stock
10 mg$44.8$56In Stock
25 mg$54.4$68In Stock
50 mg$64.8$81In Stock
100 mg$84$105In Stock
200 mg$93.6$117In Stock
500 mg$103.2$129In Stock
1 g$124.8$156In Stock
1 mL x 10 mM (in DMSO)$38.4$48In Stock
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Product Introduction

Bioactivity
Description
Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
In vitro
In the EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models, oral administration of AZD9291 (5 mg/kg) effectively inhibits AKT and ERK signaling pathways as well as EGFR phosphorylation in tumors, leading to tumor regression.
In vivo
In mutant EGFR cell lines, AZD9291 effectively inhibits cell proliferation.
Kinase Assay
ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated[1].
Cell Research
AZD-9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. 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[1].
AliasAZD-9291, Mereletinib
Chemical Properties
Molecular Weight499.61
FormulaC28H33N7O2
Cas No.1421373-65-0
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: 22 mg/mL(44 mM)
DMSO: 55 mg/mL (110.09 mM)
5% DMSO+95% Saline: 4.6 mg/mL (9.21 mM, precipitation)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO/5% DMSO+95% Saline
1mg5mg10mg50mg
1 mM2.0016 mL10.0078 mL20.0156 mL100.0781 mL
5 mM0.4003 mL2.0016 mL4.0031 mL20.0156 mL
DMSO
1mg5mg10mg50mg
10 mM0.2002 mL1.0008 mL2.0016 mL10.0078 mL
20 mM0.1001 mL0.5004 mL1.0008 mL5.0039 mL
50 mM0.0400 mL0.2002 mL0.4003 mL2.0016 mL
100 mM0.0200 mL0.1001 mL0.2002 mL1.0008 mL

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