Dovitinib lactate
作者：齊岳
發(fā)布時(shí)間：2023-08-23
09:38:07
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：Dovitinib lactate
產(chǎn)品描述：
| 產(chǎn)品描述 | Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM). |
| 靶點(diǎn)活性 | FGFR3:5 nM |
| 體外活性 | 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] |
| 體內(nèi)活性 | 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]. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 動(dòng)物實(shí)驗(yàn) | 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]. |
| 別名 | TKI-258 lactate, CHIR-258 lactate, 多韋替尼乳酸鹽 |
| 分子量 | 482.516 |
| 分子式 | C24H27FN6O4 |
| CAS No. | 692737-80-7 |
存儲(chǔ)
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 30 mg/mL (62.17 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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