Gefitinib hydrochloride

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
10g	$250	Check With Us
50g	$750	Check With Us
100g	$1125	Check With Us

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Cat #: V3289 CAS #: 184475-55-6 (HCl salt) Purity ≥ 98%

Description: Gefitinib hydrochloride, the HCl salt of Gefitinib (formerly also known as ZD1839 or trade name: Iressa), is a potent and orally-bioavailable EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

References: Wakeling AE, et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	483.36
Molecular Formula	C₂₂H₂₅Cl₂FN₄O₃
CAS No.	184475-55-6 (HCl salt)
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: >100 mg/mLr
	Water: >4 mg/mLr
	Ethanol: N/A
Solubility In Vivo	5% DMSO+corn oil: 2.5 mg/mL
Synonyms	ZD1839 HCl; ZD 1839 HCl; ZD-1839 HCl; Gefitinib HCl; trade name: Iressa.

Protocol	In Vitro	Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.
Protocol	In Vivo	Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts.

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	1mg	5mg	10mg	20mg
1mM	2.0689 mL	10.3443 mL	20.6885 mL	41.3770 mL
5mM	0.4138 mL	2.0689 mL	4.1377 mL	8.2754 mL
10mM	0.2069 mL	1.0344 mL	2.0689 mL	4.1377 mL
20mM	0.1034 mL	0.5172 mL	1.0344 mL	2.0689 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.