Lapatinib

SKU: orb1225581

Description

A reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively; displays no significant activity against other kinases, including ErbB4, c-Src, and c-Raf1; reduces tyrosine phosphorylation of EGFR and erbB2, and inhibits activation of Erk1/2 and AKT both in vitro and in vivo; inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg; orally active.Breast Cancer Approved(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.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.Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces 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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 231277-92-2
• MW: 581.0576
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₆ClFN₄O₄S
• SMILES: CS(=O)(=O)CCNCC1=CC=C(O1)C1=CC2=C(C=C1)N=CN=C2NC1=CC(Cl)=C(OCC2=CC(F)=CC=C2)C=C1
• Target: EGFR
• Solubility: DMSO: ≥ 39 mg/mL

Bioactivity

• 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. Animal model: CD-1 nude female mice (4-6 weeks old) with HN5 cells. 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.
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• 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. 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. Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest. Western blot analysis. 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 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 Cell line: HN5 cells. Concentration: 1 μM, or 10 μM. Incubation time: 72 hours. Result: Resulted in induction of G1 arrest.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GW572016 | GW-572016 | GW 572016

Quick Database Links

Gene Symbol

EGFR