Lapatinib (free base)

Name: Lapatinib (free base)
Brand: Adooq Bioscience
SKU: A11752
Rating: 100 (7 reviews)

Catalog No.: A11752

Product Citations (7)

Lapatinib (free base) Chemical Structure

CAS NO. 231277-92-2

Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.

Availability: In stock

Package	Price	Qty
10 mg	$30.00
25 mg	$40.00
50 mg	$50.00
100 mg	$70.00
10mM * 1mL in DMSO	$50.00
Custom Size	Get quote

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Products are for laboratory research use only. Not for human use. We do not sell to patients.

Adooq Products cited in reputable paper

Publications Citing Use of Adooq Lapatinib (free base)

Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026

Biological Activity

Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.

Targets

Target	Value
ErbB2	IC50: 9.2nM
EGFR	IC50: 10.8nM
ErbB4	IC50: 367nM
c-Src	IC50: 3.5μM
C-Raf-1	IC50: >10μM
MEK	IC50: >10μM
ERK	IC50: >10μM
c-Fms	IC50: >10μM
CDK1	IC50: >10μM
CDK2	IC50: >10μM
p38	IC50: >10μM
Tie-2	IC50: >10μM
VEGFR2	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	99 mg/mL (170.37 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+30% PEG 300+5% Tween 80+ddH2O	9 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	17.21 mL	86.04 mL	172.09 mL
0.5 mM	3.44 mL	17.21 mL	34.42 mL
1 mM	1.72 mL	8.6 mL	17.21 mL
5 mM	0.34 mL	1.72 mL	3.44 mL

*The above data is based on the productmolecular weight 581.1 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Chemical Properties

Catalog Num	A11752
CAS No.	231277-92-2
Formula	C29H26ClFN4O4S
M. Wt	581.1
Purity	>98%
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
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.