Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 47.00 | |
10 mg | In stock | $ 72.00 | |
25 mg | In stock | $ 131.00 | |
50 mg | In stock | $ 225.00 | |
100 mg | In stock | $ 376.00 | |
200 mg | In stock | $ 563.00 | |
500 mg | In stock | $ 888.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 52.00 |
Description | Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM). |
Targets&IC50 | FGFR3:5 nM |
In vitro | ALL cells were extremely sensitive to TKI258 treatment with a concentration for 50% inhibition of cell proliferation (IC50) values in the nanomolar range in vitro.?By combination with mTOR inhibitor RAD001, a synergistic effect on cell death and cell proliferation was observed in these cells[1].Treatment of SK-HEP1 cells with dovitinib resulted in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibited basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2[2] |
In vivo | In vivo, dovitinib potently inhibited tumor growth of six HCC lines.?Inhibition of angiogenesis correlated with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways.?Dovitinib also caused dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which resulted in a reduction in cellular proliferation and the induction of tumor cell apoptosis.?In an orthotopic model, dovitinib potently inhibited primary tumor growth and lung metastasis and significantly prolonged mouse survival[2]. |
Cell Research | Determination of cell proliferation by 3,[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) assay.?Different leukemic cells were seeded into a 96-well plate at a density of 5×10^3 cells per well and exposed to different concentrations of TKI258, with or without RAD001, in culture medium.?After incubation for indicated time points.Cell-cycle analysis:For cell-cycle analysis, cells were exposed to different concentrations of TKI258, with or without RAD001, in growth medium.?After different culture durations, cells were harvested and fixed in 70% ethanol at 4°C for over 30 min. After incubation for indicated time points, DNA contents were stained.Apoptosis analysis:Cell apoptosis was detected by determining phosphatidylserine expression on the cell surface[1]. |
Animal Research | 21-0208 and SK-HEP1 cells as well as patient-derived HCC models were employed to study the antitumor effect of dovitinib.?Changes of biomarkers relevant to FGFR/VEGFR/PDGFR pathways were determined by Western blotting.?Microvessel density, apoptosis and cell proliferation were analyzed by immunohistochemistry[1]. |
Synonyms | TKI-258 lactate, CHIR-258 lactate |
Molecular Weight | 482.51 |
Formula | C24H27FN6O4 |
CAS No. | 692737-80-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 30 mg/mL (62.17 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Dovitinib lactate 692737-80-7 Angiogenesis Tyrosine Kinase/Adaptors PDGFR c-Kit VEGFR FGFR FLT TKI-258 lactate CHIR-258 Dovitinib SCFR CD117 Platelet-derived growth factor receptor TKI258 TKI 258 CHIR258 CHIR-258 lactate CD135 FLT3 CHIR 258 Fms like tyrosine kinase 3 Inhibitor Cluster of differentiation antigen 135 Vascular endothelial growth factor receptor inhibit TKI-258 Fibroblast growth factor receptor inhibitor