Lapatinib Ditosylate is a selective and effective inhibitor of ErbB-2 and EGFR dual tyrosine kinases. ErbB-2 and EGFR dual tyrosine kinases are growth promoting factors that are over expressed in some breast cancer cell lines. Lapatinib inhibits the growth of both EGFR- and ErbB-2-overexpressing cells, whereas OSI-774 and Iressa which are EGFR selective inhibitors preferentially inhibit the growth of the EGFR-overexpressing cell lines. Research studies have reported that Lapatinib Ditosylate can inhibit breast cancer cell proliferation.
Cell Death Dis. 2021 Feb 15;12(2):179.
Targeting transcription of MCL-1 sensitizes HER2-amplified breast cancers to HER2 inhibitors
Lapatinib Ditosylate purchased from AbMole
Proc Natl Acad Sci U S A. 2018 Feb 23.
Coamplification of miR-4728 protects HER2-amplified breast cancers from targeted therapy
Lapatinib Ditosylate purchased from AbMole
J Pharm Pharm Sci. 2016 Feb;404-407.
Phase dependent discrepancy in murine vaginal micro-environment: A correlative analysis of PH, glycogen and Serum Estrogen upon exposure to Lapatinib Ditosylate
Lapatinib Ditosylate purchased from AbMole
Cell Experiment | |
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Cell lines | HFF; BT474, MCF-7, N87, and CaLu-3; HN5, A-431, T47D, HB4a, and HB4a c5.2 cell lines |
Preparation method | In Vitro Growth Inhibition Assays For assessment of cell-based potency, cells were plated in 96-well Falcon plates (Becton Dickinson) in the growth media described above. Plating densities that resulted in logarithmic growth of vehicle-treated cells for the duration of the assay were used: HFF, 15,000 cells/cm2; BT474, MCF-7, N87, and CaLu-3, 30,000 cells/cm2; and HN5, A-431, T47D, HB4a, and HB4a c5.2, 10,000 cells/cm2. After 24 h, cells were exposed to compounds at the concentrations indicated in Fig. 2. HFF, BT474, HN5, and N87 cells were treated in low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. MCF-7 cells were treated in 50% high-glucose DMEM, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. T47D, A-431, and CaLu-3 cells were treated in 50% RPMI, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. HB4a and HB4a c5.2 cells were treated in 50% DMEM, 50% RPMI 1640 supplemented with 5% FBS, 2.5 μg/ml hydrocortisone, 2.5 μg/ml insulin, 25 μg/ml hygromycin B, 50 μg/ml gentamicin, and 0.3% v/v DMSO. After 3 days, relative cell number was estimated using methylene blue staining. The media were removed, and 100 μl of 0.5% w/v methylene blue dissolved in 50% ethanol and 50% water were added to each well. Plates were washed by immersion in deionized water and allowed to air dry. 1% w/v n-lauroylsarcosine (100 μl) dissolved in PBS was added to each well, and plates were incubated for 30 min at room temperature. The absorbance at 620 nm was read in a Spectra (Tecan) microplate reader. Data were analyzed using curve-fitting macros written for Microsoft Excel. Concentrations with IC50 were interpolated using the method of Levenberg and Marquardt and this equation: y = Vmax × [1 − (xn/(Kn + xn))], where “K” is equal to IC50. |
Concentrations | 0~100 μM |
Incubation time | 3 days |
Animal Experiment | |
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Animal models | CD-1 nude female mice were used for HN5 human tumor xenografts, C.B-17 SCID female mice were used for BT474 human tumor xenografts |
Formulation | sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10) |
Dosages | 30 or 100 mg/kg twice daily for 21 days |
Administration | p.o. |
Molecular Weight | 925.46 |
Formula | C29H26ClFN4O4S.2C7H8O3S |
CAS Number | 388082-78-8 |
Solubility (25°C) | DMSO 90 mg/mL |
Storage | -20°C, sealed, protect from light |
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.
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