Osimertinib (Synonyms: AZD-9291; Mereletinib)

Cat. No.: HY-15772 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Osimertinib (AZD9291) 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, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

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

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 66	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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Customer Review

Based on 82 publication(s) in Google Scholar

Other Forms of Osimertinib:

71 Publications Citing Use of MCE Osimertinib

Proliferation Assay

: Osimertinib purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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

12 nM (IC₅₀, Enzyme assays)

EGFR^L858R/T790M

1 nM (IC₅₀, Enzyme assays)

In Vitro

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC₅₀s of 41, 26, 41, and 31 nM, respectively^[2].
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC₅₀s of 6, 7, and 74 nM, respectively^[2].
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC₅₀ ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)^[2].
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC₅₀ of 8 nM in PC-9) and T790M (mean IC₅₀s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC₅₀s of 650 and 461 nM in Calu3 and H2073 respectively)^[1].
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) ^[2].

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

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 (IC₅₀s=6, 7, 74 nM, respectively)

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 (IC₅₀s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:	Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation (IC₅₀s=16, 701, 230, 38 nM, respectively)

Apoptosis Analysis^[2]

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

In Vivo

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1].

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 days
Result:	Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Clinical Trial

Molecular Weight

499.61

Appearance

Solid

Formula

C₂₈H₃₃N₇O₂

CAS No.

1421373-65-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (125.10 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0016 mL	10.0078 mL	20.0156 mL
5 mM	0.4003 mL	2.0016 mL	4.0031 mL
10 mM	0.2002 mL	1.0008 mL	2.0016 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 0.5%HPMC 1%Tween80
Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60°C
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution
3.

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (284 KB) SDS (252 KB)

COA (255 KB) HNMR (286 KB) LCMS (265 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]. 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]

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.

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Keywords:

Osimertinib1421373-65-0AZD-9291 MereletinibAZD9291AZD 9291EGFREpidermal growth factor receptorErbB-1HER1PC-9H1975Ba/F3 cellscancertumor xenograft modelInhibitorinhibitorinhibit

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Osimertinib (Synonyms: AZD-9291; Mereletinib)

Customer Review

Other Forms of Osimertinib:

71 Publications Citing Use of MCE Osimertinib

Featured Recommendations

•Related Screening Libraries:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

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The molarity calculator equation

The dilution calculator equation

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