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Erlotinib mesylate

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Erlotinib mesylate
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Cat #: V3252 CAS #: 248594-19-6 (mesylate); 183319-69-9 (HCl); 183321-74-6 (free base) Purity ≥ 98%

Description: Erlotinib mesylate (also known as OSI-744 mesylate, trade name: Tarceva) is the mesylate salt of erlotinib which is an EGFR (epidermal growth factor receptor) inhibitor with IC50 of 2 nM in cell-free assays, and is >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

References: Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57(21):4838-48.

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Molecular Weight (MW)393.44
Molecular FormulaC23H27N3O7S
CAS No.248594-19-6 (mesylate); 183319-69-9 (HCl); 183321-74-6 (free base)
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: > 10mMr
Water: N/Ar
Ethanol: N/A
SMILES CodeCOCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC.CS(=O)(O)=O
SynonymsCP358774 mesylate; NSC 718781 mesylate; CP358774 mesylate, NSC 718781 mesylate; CP-358,774 mesylate; CP-358774 mesylate; OSI-774 mesylate; OSI 774 mesylate; OSI774 mesylate; Erlotinib mesylate
ProtocolIn VitroErlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 of 100 nM for an 8-day proliferation assay.
In VivoThere is a 1.49-fold statistically significant difference between AUC0-inf after p.o. administration of Erlotinib (5 mg/kg) comparing Bcrp1/Mdr1a/1b-/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL respectively, P=0.01).
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
1mM2.5417 mL12.7084 mL25.4168 mL50.8337 mL
5mM0.5083 mL2.5417 mL5.0834 mL10.1667 mL
10mM0.2542 mL1.2708 mL2.5417 mL5.0834 mL
20mM0.1271 mL0.6354 mL1.2708 mL2.5417 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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

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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.