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[CAS NO. 388082-77-7]  Lapatinibditosylate

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PRODUCTS SPECIFICATIONS [388082-77-7]

Catalog
HY-50898A
Brand
MCE
CAS
388082-77-7

DESCRIPTION [388082-77-7]

Overview

MDLMFCD09264195
Molecular Weight925.46
Molecular FormulaC43H42ClFN4O10S3
SMILESO=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O

For research use only. We do not sell to patients.

53 Publications Citing Use of MCE


Summary

Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC 50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively [1] .


IC50 & Target

EGFR

10.8 nM (IC 50 , Cell Free Assay)

ErbB2

9.2 nM (IC 50 , Cell Free Assay)


In Vitro

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner [1] .
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines [1] .
Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: BT474 and HN5 cells
Concentration: 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time: 6 hours
Result: Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay [1]

Cell Line: HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time: 72 hours
Result: Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis [1]

Cell Line: HN5 cells
Concentration: 1 µM, or 10 µM
Incubation Time: 72 hours
Result: Resulted in induction of G1 arrest.

In Vivo

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 nude female mice (4-6 weeks old) with HN5 cells [1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Oral administration; twice daily; for 21 days
Result: Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01283789 University of Kansas Medical Center|Novartis|GlaxoSmithKline
Metastatic Breast Cancer
February 2011 Phase 2
NCT01395537 Case Comprehensive Cancer Center
Adenocarcinoma of the Esophagus|Adenocarcinoma of the Gastroesophageal Junction
August 2011 Phase 1|Phase 2
NCT00662636 Mayo Clinic|National Cancer Institute (NCI)
Unspecified Adult Solid Tumor, Protocol Specific
August 2008 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 135.07 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0805 mL 5.4027 mL 10.8054 mL
5 mM 0.2161 mL 1.0805 mL 2.1611 mL
10 mM 0.1081 mL 0.5403 mL 1.0805 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, 4-methylbenzenesulfonate (1:2)
4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, bis(4-methylbenzenesulfonate)
Lapatinib ditosylate
GW 572016F
Tykerb

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