All AbMole products are for research use only, cannot be used for human consumption.
Crizotinib (PF-02341066) is a potent, orally bioavailable, ATP-competitive small-molecule inhibitor of c-Met kinase and ALK (anaplastic lymphoma kinase) with IC50 values to be 4 and 25 nM for C-Met and ALK resepectively.PF-2341066 (Crizotinib) potently inhibited cell proliferation, which was associated with G1-S–phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells (IC50 values=30 nM) but not ALK-negative lymphoma cells. The induction of apoptosis was confirmed using terminal deoxyribonucleotide transferase–mediated nick-end labeling and Annexin V staining (IC50 values=25–50 nM).
Cancers (Basel). 2021 Jul 9;13(14):3441.
Generation and Characterization of a New Preclinical Mouse Model of EGFR-Driven Lung Cancer with MET-Induced Osimertinib Resistance
Crizotinib purchased from AbMole
Biomed Chromatogr. 2020 Apr 23;e4863.
A Novel LC-MS/MS Method for the Determination of Ziritaxestat in Rat Plasma and Its Pharmacokinetic Study
Crizotinib purchased from AbMole
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Source | Drug Des Devel Ther (2015). Figure 2. PF-2341066 |
| Method | Matrigel invasion assay | |
| Cell Lines | NPC cell | |
| Concentrations | 0.67±0.07 mm | |
| Incubation Time | 48 h | |
| Results | Distance of NPC cell scramble at 48 hours was 0.99±0.11 mm in plates of PF-2341066 alone, 0.67±0.07 mm in cisplatin alone, and 0.33±0.05 mm in combination, (P,0.05) |
 |
Source | Drug Des Devel Ther (2015). Figure 1. PF-2341066 |
| Method | Cell proliferation assay | |
| Cell Lines | HNE -1 cells | |
| Concentrations | 0.79±0.21 μmol/L | |
| Incubation Time | 48 h | |
| Results | The half maximal inhibitory concentration of PF-2341066 alone is 0.79±0.21 μmol/L, while combination with cisplatin is 0.41±0.13 μmol/L. The inhibition rate increased by 23.4% and showed certain synergistic effects |
| Cell Experiment | |
|---|---|
| Cell lines | Karpas299, SUDHL-1, or U-937 cells |
| Preparation method | Cell Proliferation/Survival Assays. Cells were seeded in 96-well plates at low density at 37°C in medium supplemented with 10% FBS (growth medium) and after 24 h were switched to low serum medium (2% FBS). Designated concentrations of PF-2341066 were added to each well and cells were incubated at 37°C for 72 h. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay (Promega) was done to determine the relative cell numbers. IC50 values were calculated by concentration-response curve fitting using a Microsoft Excel–based four-parameter analytic method. |
| Concentrations | 0~1µM |
| Incubation time | 72h |
| Animal Experiment | |
|---|---|
| Animal models | S.c. Xenograft Models in Athymic Mice |
| Formulation | sterile water |
| Dosages | 100mg/kg daily |
| Administration | oral gavage |
| Molecular Weight | 450.34 |
| Formula | C21H22Cl2FN5O |
| CAS Number | 877399-52-5 |
| Solubility (25°C) | DMSO 11 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Foyil KV, et al. Cancer J. Brentuximab vedotin and crizotinib in anaplastic large-cell lymphoma.
| Related c-Met Products |
|---|
| AMG-208
AMG-208 is a potent small molecular inhibitor c-Met with an IC50 of 9.3 nM. AMG-208 is also a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity. |
| BMS-777607
BMS-777607 is a selective and potent small-molecule met kinase inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively. |
| BMS 794833
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor. |
| AMG-458
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively. |
| XL-184
Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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