Lapatinib

SKU: orb1310962

Description

Lapatinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 231277-92-2
• MW: 581.06
• Purity: 99.89%
• Formula: C₂₉H₂₆ClFN₄O₄S
• SMILES: N(C=1C2=C(C=CC(=C2)C=3OC(CNCCS(C)(=O)=O)=CC3)N=CN1)C4=CC(Cl)=C(OCC5=CC(F)=CC=C5)C=C4
• Target: Ferroptosis,Autophagy,EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:9.3 mg/mL (16.01 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:262.5 mg/mL (451.76 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HER1:10.2 nM|SKBR3 cells:0.080 ± 0.0173 μM|HCC1954 cells:2.67 ± 0.08 μM|BT-474 cells:0.036 ± 0.0151 μM|MDA-MB-453 cells:6.08 ± 0.825 μM|MDA-MB-231 cells:7.46 ± 0.102 μM|HER2:9.8 nM|EFM-192A cells:0.193 ± 0.0665 μM
• In Vivo:
  METHODS: To detect anti-tumor activity in vivo, Lapatinib (100 mg/kg) was administered intraperitoneally once daily for three weeks to CD-1 athymic nude mice bearing human gastric cancer tumor N87. RESULTS: Lapatinib caused tumor regression in N87 xenografts. METHODS: To detect in vivo antitumor activity, Lapatinib (30-100 mg/kg administered by gavage twice daily for 21 days) and Topoteca (6-10 mg/kg administered intraperitoneally three times every four days) were administered by gavage to SCID mice harboring human mammary carcinoma tumor BT474. RESULTS: The combination of Lapatinib and Topoteca showed enhanced efficacy in ER2+BT474 xenografts.
• In Vitro:
  METHODS: Fourteen human gastric and esophageal cancer cell lines were treated with Lapatinib (0.3125-10 µmol/L) for 6 days, and the cell counts were measured by particle counter. RESULTS: N87, OE19, NUGC4, NUGC3, FU97, and SNU16 cells were sensitive to Lapatinib with IC50s of 0.01, 0.09, 0.35, 2.24, 4.86, and 8.58 μmol/L, respectively. METHODS: Human breast cancer cells MDA-MB-231 and SK-BR-3 were treated with Lapatinib (0.5-2 µM) for 48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: The expression of PKM2 was significantly reduced in both MDA-MB-231 and SK-BR-3 cell lines treated with 1.0 µM Lapatinib compared to lower concentrations.
• Cell Research:
  Cells are plated in 96-well plates, in the media, at the following densities: HFF and HN5, 1000 cells/well and BT474, 5000 cells/well. After 24 h, the cells are exposed to vehicle (0.3% DMSO) or Lapatinib (1 nM, 10 nM, 100 nM, 1μM, 10μM, and 100μM). Lapatinib is removed from the cells after 72 h and is replaced by either DMEM containing 10% FBS and 50 μg/mL Gentamicin (HFF and HN5) or RPMI containing 10% FBS and 50 μg/mL Gentamicin (BT474). Methylene blue staining is performed at the time points over a total period of 16 days. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide .
• Animal Research:
  CD-1 nude female mice are used for HN5 human tumor xenografts, which are initiated by injection of a cell suspension in PBS: Matrigel (1:1). C.B-17 SCID female mice are used for BT474 human tumor xenografts, which are initiated by implantation of tumor fragments (20-100 mg) from established tumors. Tumor cells and fragments are implanted by s.c. injection in the right flank. The s.c. tumors are measured with calipers, and mice are weighed twice weekly. Tumor weight is estimated from tumor volume using this formula: length×width2/2=tumor volume (mm3). Treatment begins when tumors are palpable, 3-5 mm in diameter. Lapatinib (30 and 100 mg/kg) is administered p.o. twice daily for 21 days in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, inhibit, Inhibitor, HER2/ErbB2, HER1, Lapatinib, Ferroptosis, Epidermal growth factor receptor, ErbB-1, EGFR, GSK 572016, GSK572016, GSK-572016, GW572016, GW-572016, GW2016, GW-2016, GW 2016, GW 572016

Compound Identifiers

PubChem CID

208908