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Osimertinib [1421373-65-0]

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Référence NB-64-14150-100mg

Conditionnement : 100mg

Marque : Neo Biotech

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Osimertinib

(Synonyms: Mereletinib, AZD-9291) Copy Product Info

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Synonyms: Mereletinib, AZD-9291

Catalog No. T2490 Copy Product Info

Purity: 99.83%

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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.

Cas No. 1421373-65-0

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.83%

Appearance:Solid

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.
Targets & IC50	MNK1:324 nM, H1975 cells:1.78 μM, MNK2:48.6 nM, EGFR (WT):493.8 nM, PC9 cells:0.66 μM, EGFR (exon 19 deletion):12.92 nM, EGFR (L858R/T790M):11.44 nM
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.
Synonyms	Mereletinib, AZD-9291
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].

Chemical Properties

Molecular Weight	499.61
Formula	C₂₈H₃₃N₇O₂
Cas No.	1421373-65-0
Smiles	CN1C=C(C=2C1=CC=CC2)C3=NC(NC4=C(OC)C=C(N(CCN(C)C)C)C(NC(C=C)=O)=C4)=NC=C3
Relative Density.	1.19 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 22 mg/mL (44.03 mM), Sonication is recommended.

DMSO: 120 mg/mL (240.19 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9.2 mg/mL (18.41 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0016 mL	10.0078 mL	20.0156 mL	100.0781 mL
5 mM	0.4003 mL	2.0016 mL	4.0031 mL	20.0156 mL
10 mM	0.2002 mL	1.0008 mL	2.0016 mL	10.0078 mL
20 mM	0.1001 mL	0.5004 mL	1.0008 mL	5.0039 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0400 mL	0.2002 mL	0.4003 mL	2.0016 mL
100 mM	0.0200 mL	0.1001 mL	0.2002 mL	1.0008 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

tumor xenograft modelPC-9OsimertinibInhibitorinhibitHER1H1975ErbB-1Epidermal growth factor receptorEGFR (L858R/T790M)EGFR (Exon 19 deletion)EGFRcancerBa/F3 cellsAZD9291AZD 9291

Related Tags: Osimertinib chemical structure | Osimertinib in vivo | Osimertinib in vitro | Osimertinib formula | Osimertinib molecular weight