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Lapatinib ditosylate monohydrate

Catalog No. T0078L CAS 388082-78-8

Synonyms: Lapatinib ditosylate monohydrate, Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate hydrate, Lapatinib tosilate, Tykerb, Tyverb

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

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Lapatinib ditosylate monohydrate Chemical Structure

Lapatinib ditosylate monohydrate, CAS 388082-78-8

Pack Size	Availability	Price/USD
50 mg	In stock	$ 48.00
100 mg	In stock	$ 64.00
200 mg	In stock	$ 95.00

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Purity: 99%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.
Targets&IC50	EGFR:10.8 nM, ERB4:367 nM, ErbB2:9.2 nM
Kinase Assay	In vitro kinase assays: The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.

Synonyms	Lapatinib ditosylate monohydrate, Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate hydrate, Lapatinib tosilate, Tykerb, Tyverb
Molecular Weight	943.47
Formula	C29H26ClFN4O4S·2(C7H8O3S)·H2O
CAS No.	388082-78-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 91 mg/mL(96.5 mM)

References and Literature

1. Rusnak DW, et al. Mol Y Ther, 2001, 1(2), 85-94.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library FDA-Approved Kinase Inhibitor Library

Related Products

Related compounds with same targets

Tyrphostin A25 EGFR-IN-11 EGFR-IN-1 hydrochloride Tyrphostin AG 112 RG13022 PD168393 PD 174265 SYR127063

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Keywords

Lapatinib ditosylate monohydrate 388082-78-8 Angiogenesis Apoptosis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors Ferroptosis EGFR Lapatinib ditosylate HER1 Lapatinib ditosylate Monohydrate ErbB-1 GW2016 ditosylate Lapatinib Lapatinib ditoluenesulfonate monohydrate Lapatinib tosilate hydrate Lapatinib tosilate GW572016 ditosylate Lapatinib ditoluenesulfonate Monohydrate Lapatinib tosilate Hydrate Tykerb inhibit Lapatinib Ditosylate Tyverb Lapatinib ditoluenesulfonate Epidermal growth factor receptor Inhibitor inhibitor

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