Lapatinib ditosylate monohydrate

SKU: orb1225136

Description

Lapatinib ditosylate is an anti-Y drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung Y.(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.

Key Properties

• CAS Number: 388082-78-8
• MW: 943.47
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₆ClFN₄O₄S·2(C₇H₈O₃S)·H₂O
• SMILES: O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.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.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: Soluble in DMSO

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.
• 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.

Storage & Handling

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

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Gene Symbol

EGFR