Osimertinib mesylate (Synonyms: AZD-9291 mesylate; Mereletinib mesylate)

Name: Osimertinib mesylate
Brand: MedChemExpress
SKU: HY-15772A
Rating: 5.0 (101 reviews)

Cat. No.: HY-15772A Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

For research use only. We do not sell to patients.

Osimertinib mesylate Chemical Structure

CAS No. : 1421373-66-1

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Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
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Based on 101 publication(s) in Google Scholar

Other Forms of Osimertinib mesylate:

90 Publications Citing Use of MCE Osimertinib mesylate

Proliferation Assay

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]; U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]; Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]; U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595. [Abstract]; MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]; Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]; Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]; Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]; Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]; In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]; In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

: Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]; Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR^L858R/T790M

1 nM (IC₅₀)

EGFR^L858R

12 nM (IC₅₀)

In Vitro

Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC₅₀ values ranging from 13 to 54 nM for Osimertinib. Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC₅₀ potency less than 15 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	PC-9, H3255, PC-9ER, and H1975 cells
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Dramatically inhibited cell proliferation (IC₅₀=41,26, 41, 31 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:	Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation (IC₅₀ = 6, 7, 74 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:	Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation (IC₅₀ = 16, 701, 230, 38 nM, respectively)

Apoptosis Analysis^[2]

Cell Line:	Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M) ^[2]
Concentration:	0.1 μM
Incubation Time:	48 hours
Result:	Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.

In Vivo

The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib, while 5 of 5 mice treated with vehicle shows tumor growth^[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1]
Dosage:	0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration:	p.o.; daily for 14 day
Result:	Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Clinical Trial

Molecular Weight

595.71

Formula

C₂₉H₃₇N₇O₅S

CAS No.

1421373-66-1

Appearance

Solid

Color

White to yellow

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 13.89 mg/mL (23.32 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6787 mL	8.3933 mL	16.7867 mL
5 mM	0.3357 mL	1.6787 mL	3.3573 mL
10 mM	0.1679 mL	0.8393 mL	1.6787 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

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

[2]. [2]Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6787 mL	8.3933 mL	16.7867 mL	41.9667 mL
	5 mM	0.3357 mL	1.6787 mL	3.3573 mL	8.3933 mL
	10 mM	0.1679 mL	0.8393 mL	1.6787 mL	4.1967 mL
	15 mM	0.1119 mL	0.5596 mL	1.1191 mL	2.7978 mL
	20 mM	0.0839 mL	0.4197 mL	0.8393 mL	2.0983 mL

Osimertinib mesylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Osimertinib1421373-66-1AZD-9291MereletinibAZD9291AZD 9291EGFREpidermal growth factor receptorErbB-1HER1PC-9H1975Ba/F3 cellscancertumor xenograft modelInhibitorinhibitorinhibit

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Osimertinib mesylate (Synonyms: AZD-9291 mesylate; Mereletinib mesylate)

Customer Review

Other Forms of Osimertinib mesylate:

Osimertinib mesylate Related Antibodies

90 Publications Citing Use of MCE Osimertinib mesylate

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•Related Screening Libraries:

•Related Small Molecules:

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View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Osimertinib mesylate Related Antibodies

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Complete Stock Solution Preparation Table

Osimertinib mesylate Related Classifications

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