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Dovitinib lactate

Catalog No. T7104 CAS 692737-80-7

Synonyms: CHIR-258 lactate, TKI-258 lactate, 多韦替尼乳酸盐

Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).

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Dovitinib lactate, CAS 692737-80-7

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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	CHIR-258 lactate, TKI-258 lactate, 多韦替尼乳酸盐
Molecular Weight	482.516
Formula	C24H27FN6O4
CAS No.	692737-80-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 30 mg/mL (62.17 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Eucker J , Zang C , Zhou Y , et al. TKI258, a Multi-tyrosine Kinase Inhibitor Is Efficacious Against Human Infant/Childhood Lymphoblastic Leukemia In Vitro[J]. Anticancer research, 2014, 34(9):4899-4907. 2. Huynh H , Chow P K H , Tai W M , et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma[J]. Journal of Hepatology, 2012, 56(3):0-601.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Lung Cancer Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Angiogenesis related Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

SU14813 maleate Imatinib impurities3 Dovitinib Dilactic Acid Dovitinib (TKI258) Lactate PD180970 c-Kit-IN-5-1 PLX647 Agerafenib hydrochloride

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Dovitinib lactate 692737-80-7 蛋白酪氨酸激酶血管生成 c-Kit FGFR FLT PDGFR VEGFR 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

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