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OSIMERTINIB DIMESYLATE

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OSIMERTINIB DIMESYLATE
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Size Price Stock
1g$350Check With Us
2g$550Check With Us
5g$930Check With Us
email: [email protected]        [email protected]

Cat #: V3976 CAS #: 2070014-82-1 Purity ≥ 98%

Description: Osimertinib dimesylate (mereletinib; AZD 9291; AZD9291; AZD-9291; trade name Tagrisso), the dimesylate salt of osimertinib, is an oral bioavailable and covalent/irreversible EGFR inhibitor approved as a cancer treatment in 2017 by both the Food and Drug Administration and the European Commission.

References: 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.

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Molecular Weight (MW)691.82
Molecular FormulaC₃₀H₄₁N₇O₈S₂
CAS No.2070014-82-1
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: <1 mg/mLr
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo1% DMSO+30% PEG 300+dd H2O: 30mg/mL
SynonymsAZD-9291 dimesylate; AZD9291; AZD 9291; Mereletinib dimesylate; Trade name: Tagrisso
ProtocolIn VitroOsimertinib (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 (AZD-9291). 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.
In VivoThe 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 (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.4455 mL7.2273 mL14.4546 mL28.9093 mL
5mM0.2891 mL1.4455 mL2.8909 mL5.7819 mL
10mM0.1445 mL0.7227 mL1.4455 mL2.8909 mL
20mM0.0723 mL0.3614 mL0.7227 mL1.4455 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
 
=
Concentration
 
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Volume
 
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
 
×
 
Volume(start)
V1
 
=
 
Concentration(final)
C2
 
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Volume(final)
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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.