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Lapatinib (GW572016) EGFR/HER2 Inhibitor

Cat.No.S2111

Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

Lapatinib (GW572016) EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 581.06

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	VEGFR FGFR PDGFR c-Met Src MEK CSF-1R HER2 FLT3 c-Kit
Other EGFR Inhibitors	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) Genistein Poziotinib (NOV120101, HM781-36B) Rociletinib (CO-1686) WZ4002

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 100 mg/mL (172.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (172.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (172.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (172.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (172.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about Lapatinib (GW572016) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about Lapatinib (GW572016) working concentrations for cell culture treatment

Lapatinib (GW572016) is a potent inhibitor of HER2 (10.2 nM), EGFR kinase (0.13 µM), HER2 kinase (0.037 µM), HER2 inhibition (109 nmol/L), EGFR (3 nM), human mPGES-1 (0.8 µM), mouse mPGES-1 (12 µM), β-haematin (5.43 ± 0.03 µM), EGFR/HER1 (10.8 nM), HER4 (367 nM), HER2 enzyme (9.2 nM), ER (>3000 nM), MAPK pathway, PI3K pathway, AKT, Erk1/2, PTTG, PP2A, SRC, FAK, mTORC1, AXL, Casein kinase II, CDKN1B, NFKB, IRS1, IRS4, PIK3CA, PTEN, FGFR, ABCB1, ABCG2, Glycolytic enzymes, HER3, RON, p95HER2. Lapatinib (GW572016) exhibits the greatest inhibitory potency toward EGFR (IC50 = 3 nM).

Read more about selectivity & specificity

Mechanism of Action

Information	Lapatinib (GW572016) is a potent, reversible dual EGFR and HER2 tyrosine kinase inhibitor. It affects PI3K/AKT/mTOR and MAPK/ERK signaling pathways by blocking receptor autophosphorylation, inhibiting tumor cell proliferation and promoting apoptosis.
Read more about Lapatinib (GW572016) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about Lapatinib (GW572016) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	581.06	Formula	C₂₉H₂₆ClFN₄O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	231277-92-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GSK572016, GW2016			Smiles	CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

Read more about storage & stability

Read more comparative analysis about Lapatinib (GW572016)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
If I want to use this compound via injection in tumor-bearing mice, how could I prepare the solution?

Answer:
For I.P. administration, the compound solution should be clear solution. It can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):