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Lapatinib

Cat. No. M3517
Lapatinib Structure
Synonym:

GW-572016

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
25mg USD 25  USD25 In stock
50mg USD 45  USD45 In stock
100mg USD 70  USD70 In stock
500mg USD 145  USD145 In stock
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Quality Control
Biological Activity

Lapatinib is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively. Lapatinib is >300-fold selective for EGFR and ErbB-2 over other kinases tested such as c-Src, MEK and ERK, except for ErbB-4. Lapatinib prevents receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner with IC50 of 0.17 and  0.08 μM against BT474 and HN5 cell lines, respectively.  The ability of Lapatinib to blocks EGFR and ErbB-2 autophosphorylation in EGFR- and ErbB-2-overexpressing tumor cells is ∼10-fold less than its potency on the purified enzyme. The ErbB-2-transfected mammary epithelial cell line, HB4a c5.2, is ∼40-fold more responsive to Lapatinib treatment than the untransfected parental control line, HB4a. Transient exposure to 30 μM Lapatinib results in complete inhibition of outgrowth of the HN5 cell population after ∼2 additional weeks of culture without Lapatinib. Lapatinib  inhibits tumor growth by 50% occurs at concentrations of >3.3 μM. Significant prevention of outgrowth (20%) occurs at doses as low as 0.37 μM. Lapatinib is similar to OSI-774 in its ability to inhibit outgrowth of the EGFR-overexpressing cell line. Lapatinib is potent at inhibiting the growth of BT474 and HN5 human tumor xenografts. A dose-responsive inhibition of both models occurs on treatment of tumor-bearing mice with 30 and 100 mg/kg Lapatinib orally, twice daily. Lapatinib at the dose of the 100 mg/kg completely inhibits the growth of tumor. At this dose, there is <10% weight loss in treated animals over the course of the 21-day treatment. Lapatinib has been approved for HER-2-positive metastatic breast cancer. Lapatinib has entered in a phase III clinical trial for the treatment of HER2+ metastatic breast cancer.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Cell (2015). Figure 3. Lapatinib (Abmole)
Method Immunoblotting
Cell Lines BT-474, SKBR3 cell
Concentrations 1µM
Incubation Time 24 h
Results This led to the loss of p110b recruitment and the block of the rebound of AKT activation observed 24 hr after treatment with BYL719 alone.
Protocol
Cell Experiment
Cell lines HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
Preparation method Exposing cells to various concentrations of Lapatinib for 72 hours. Using methylene blue stainingto estimate relative cell number . 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.
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation time 72 hours
Animal Experiment
Animal models CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
Formulation Formulated in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
Dosages ~100 mg/kg
Administration Orally twice daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 581.06
Formula C29H26ClFN4O4S
CAS Number 231277-92-2
Purity 99.80%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Binghe Xu, et al. Pyrotinib plus capecitabine versus lapatinib plus capecitabine for the treatment of HER2-positive metastatic breast cancer (PHOEBE): a multicentre, open-label, randomised, controlled, phase 3 trial

[2] Fei Ma, et al. Pyrotinib or Lapatinib Combined With Capecitabine in HER2-Positive Metastatic Breast Cancer With Prior Taxanes, Anthracyclines, and/or Trastuzumab: A Randomized, Phase II Study

[3] Minna Voigtlaender, et al. Lapatinib

[4] Minna Nolting, et al. Lapatinib

[5] Cynthia Frankel, et al. Lapatinib side-effect management

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  Catalog
Abmole Inhibitor Catalog




Keywords: Lapatinib, GW-572016 supplier, EGFR/HER2, inhibitors

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