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[CAS NO. 231277-92-2]  Lapatinib

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PRODUCTS SPECIFICATIONS [231277-92-2]

Catalog
HY-50898
Brand
MCE
CAS
231277-92-2

DESCRIPTION [231277-92-2]

Overview

MDLMFCD09264194
Molecular Weight581.06
Molecular FormulaC29H26ClFN4O4S
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

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

53 Publications Citing Use of MCE


Summary

Lapatinib (GW572016) 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

10.2 nM (IC 50 , Cell Free Assay)

ErbB2

9.8 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
NCT04591431 Fondazione per la Medicina Personalizzata
Breast Cancer|Gastrointestinal Cancer|Non Small Cell Lung Cancer|Other Cancer
October 7, 2020 Phase 2
NCT00558103 GlaxoSmithKline
Neoplasms, Breast
December 2007 Phase 2
NCT02101905 National Cancer Institute (NCI)
Anaplastic Astrocytoma|Anaplastic Ependymoma|Anaplastic Oligodendroglioma|Gliosarcoma|Mixed Glioma|Recurrent Adult Brain Neoplasm|Recurrent Glioblastoma
March 13, 2014 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 215.12 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7210 mL 8.6050 mL 17.2099 mL
5 mM 0.3442 mL 1.7210 mL 3.4420 mL
10 mM 0.1721 mL 0.8605 mL 1.7210 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 12% SBE-beta-CD

    Solubility: 5 mg/mL (8.60 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

  • 4.

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

    Solubility: 2.08 mg/mL (3.58 mM); Suspended solution; Need ultrasonic

  • 5.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.58 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]-
N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
GW 572016
Lapatinib
4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline
GSK 572016
N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
GW 572016X
N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methanesulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
Tyverb
N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
N-[4-(3-Fluorobenzyloxy)-3-chlorophenyl]-6-[5-[[2-(methylsulfonyl)ethylamino]methyl]furan-2-yl]quinazolin-4-amine
GD 2016
Tycerb

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