Dovitinib (TKI-258)
别名: CHIR-258
Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂，在无细胞试验中对III型(FLT3/c-Kit)作用最强，IC50为1 nM/2 nM，同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs，IC50为8-13 nM，但对InsR，EGFR，c-Met，EphA2，Tie2，IGF-1R和HER2作用较弱。Phase 4。
Dovitinib (TKI-258) Chemical Structure
CAS: 405169-16-6
产品质控
批次：
纯度：
99.98%
99.98
Dovitinib (TKI-258)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Hep3B | Growth Inhibition Assay | 0.1-10 μM | 24 h | induces G2 arrest | 24238094 |
| HeLa | Growth Inhibition Assay | 0.1-10 μM | 24 h | induces G2/M arrest in a concentration-dependent manner | 24238094 |
| C666-1 | Growth Inhibition Assay | 0.1-10 μM | 48 h | induces G2/M delay in a concentration-dependent manner | 24238094 |
| CNE2 | Growth Inhibition Assay | 0.1-10 μM | 48 h | induces G2/M delay in a concentration-dependent manner | 24238094 |
| HNE1 | Growth Inhibition Assay | 0.1-10 μM | 48 h | induces G2/M delay in a concentration-dependent manner | 24238094 |
| HONE1 | Growth Inhibition Assay | 0.1-10 μM | 48 h | induces G2/M delay in a concentration-dependent manner | 24238094 |
| RT4 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| TCC-SUP | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| BFTC905 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| T24 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| RT112 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| HT1376 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| MGHU4 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| HU456 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| 5637 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| UMC3 | Cell Viability Assay | 1-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 24325461 |
| MFE-296 | Function Assay | 0.05/0.1/0.5 μM | 72 h | causes a decrease in STAT3, ERK, and AKT phosphorylation | 24495750 |
| AN3CA | Function Assay | 0.05/0.1/0.5 μM | 72 h | causes a decrease in STAT3, ERK, and AKT phosphorylation | 24495750 |
| HEC-1A | Function Assay | 0.05/0.1/0.5 μM | 72 h | causes a decrease in STAT3, ERK, and AKT phosphorylation | 24495750 |
| SEM-K2 | Apoptosis Assay | 0.1/1 μM | 24 h | induces early apoptosis of SEM-K2 cells at 0.1 μM after 24 h | 25202072 |
| Nalm-6 | Apoptosis Assay | 2 μM | 24/48 h | induces apoptosis resulting in about 72% of cell death after 24 h treatment and 81% after 48 h | 25202072 |
| HUVEC | Cell Viability Assay | 0-25 μM | 72 h | inhibits cell growth in a dose dependent manner | 23228017 |
| HMVEC | Cell Viability Assay | 0-25 μM | 72 h | inhibits cell growth in a dose dependent manner | 23228017 |
| MHCC-97H | Cell Viability Assay | 0-25 μM | 72 h | inhibits cell growth in a dose dependent manner | 23228017 |
| SMMC7721 | Cell Viability Assay | 0-25 μM | 72 h | inhibits cell growth in a dose dependent manner | 23228017 |
| Huh-7 | Apoptosis Assay | 0-12.5 μM | 24 h | sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner | 22230479 |
| Sk-Hep1 | Apoptosis Assay | 0-12.5 μM | 24 h | sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner | 22230479 |
| Hep3B | Apoptosis Assay | 0-12.5 μM | 24 h | sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner | 22230479 |
| PLC5 | Apoptosis Assay | 0-12.5 μM | 24 h | sensitizes HCC cells to TRAIL- and tigatuzumab-induced apoptosis in a dose-dependent manner | 22230479 |
| PLC5 | Cell Viability Assay | 0-15 μM | 72 h | reduces cell viability in a dose-dependent manner | 22180308 |
| Hep3B | Cell Viability Assay | 0-15 μM | 72 h | reduces cell viability in a dose-dependent manner | 22180308 |
| Sk-Hep1 | Cell Viability Assay | 0-15 μM | 72 h | reduces cell viability in a dose-dependent manner | 22180308 |
| Huh-7 | Cell Viability Assay | 0-15 μM | 72 h | reduces cell viability in a dose-dependent manner | 22180308 |
| PLC5 | Apoptosis Assay | 0-15 μM | 24 h | increases apoptotic cell death in a dose-dependent manner | 22180308 |
| Hep3B | Apoptosis Assay | 0-15 μM | 24 h | increases apoptotic cell death in a dose-dependent manner | 22180308 |
| Sk-Hep1 | Apoptosis Assay | 0-15 μM | 24 h | increases apoptotic cell death in a dose-dependent manner | 22180308 |
| Huh-7 | Apoptosis Assay | 0-15 μM | 24 h | increases apoptotic cell death in a dose-dependent manner | 22180308 |
| PLC5 | Function Assay | 0-10 μM | 24 h | causes dose-dependent DNA fragmentation | 22180308 |
| Hep3B | Function Assay | 0-10 μM | 24 h | causes dose-dependent DNA fragmentation | 22180308 |
| Sk-Hep1 | Function Assay | 0-10 μM | 24 h | causes dose-dependent DNA fragmentation | 22180308 |
| Huh-7 | Function Assay | 0-10 μM | 24 h | causes dose-dependent DNA fragmentation | 22180308 |
| RT112 | Function Assay | 500 nM | 24 h | increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases | 21119661 |
| RT4 | Function Assay | 500 nM | 24 h | increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases | 21119661 |
| MGH-U3 | Function Assay | 500 nM | 24 h | increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases | 21119661 |
| SW780 | Function Assay | 500 nM | 24 h | increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases | 21119661 |
| 97-7 | Function Assay | 500 nM | 24 h | increases the proportion of cells in G1 accompanied by a decrease in S and G2/M phases | 21119661 |
| J807C | Cell Viability Assay | 0-400 nM | 48 h | inhibits cell growth in a dose dependent manner | 15598814 |
| Y373C | Cell Viability Assay | 0-400 nM | 48 h | inhibits cell growth in a dose dependent manner | 15598814 |
| K650E | Cell Viability Assay | 0-400 nM | 48 h | inhibits cell growth in a dose dependent manner | 15598814 |
| G384D | Cell Viability Assay | 0-400 nM | 48 h | inhibits cell growth in a dose dependent manner | 15598814 |
| F384L | Cell Viability Assay | 0-400 nM | 48 h | inhibits cell growth in a dose dependent manner | 15598814 |
| NCI-H1703 | Function assay | 10 uM | 24 hrs | Inhibition of TNIK in human NCI-H1703 cells transfected with lentiviral vector 7TFP assessed as reduction of GSK3 inhibitor X activated TNIK-mediated Wnt/TCF/beta-catenin-dependent transcription at 10 uM after 24 hrs by luciferase reporter assay | ChEMBL |
| LoVo | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against Wnt/beta-catenin signalling dependent human LoVo cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay | ChEMBL |
| HCT116 | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against Wnt/beta-catenin signalling dependent human HCT116 cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay | ChEMBL |
| Huh7 | Growth Inhibition Assay | 72 h | IC50=3.980 ± 0.803 μM | 23546591 | |
| PLC/PRF5 | Growth Inhibition Assay | 72 h | IC50=3.110 ± 0.337 μM | 23546591 | |
| Hep3B | Growth Inhibition Assay | 72 h | IC50=0.892 ± 0.044 μM | 23546591 | |
| HepG2 | Growth Inhibition Assay | 72 h | IC50=1.200 ± 0.226 μM | 23546591 | |
| Huh7 | Growth Inhibition Assay | 48 h | IC50=15.007 ± 7.334 μM | 23546591 | |
| PLC/PRF5 | Growth Inhibition Assay | 48 h | IC50=16.120 ± 4.001 μM | 23546591 | |
| Hep3B | Growth Inhibition Assay | 48 h | IC50=4.223 ± 0.839 μM | 23546591 | |
| HepG2 | Growth Inhibition Assay | 48 h | IC50=2.727 ± 0.429 μM | 23546591 | |
| SW780 | Growth Inhibition Assay | 5 d | IC50=50 nM | 21119661 | |
| RT112 | Growth Inhibition Assay | 5 d | IC50=15 nM | 21119661 | |
| RT4 | Growth Inhibition Assay | 5 d | IC50=5 nM | 21119661 | |
| JMSU1 | Growth Inhibition Assay | 5 d | IC50=50 nM | 21119661 | |
| J82 | Growth Inhibition Assay | 5 d | IC50=1400 nM | 21119661 | |
| 97-7 | Growth Inhibition Assay | 5 d | IC50=1000 nM | 21119661 | |
| KMS11 | Growth Inhibition Assay | 72 h | IC50=90 nM | 15598814 | |
| KMS18 | Growth Inhibition Assay | 72 h | IC50=550 nM | 15598814 | |
| OPM2 | Growth Inhibition Assay | 72 h | IC50=90 nM | 15598814 | |
| H929 | Growth Inhibition Assay | 72 h | IC50> 2500 nM | 15598814 | |
| 8226 | Growth Inhibition Assay | 72 h | IC50> 2500 nM | 15598814 | |
| U266 | Growth Inhibition Assay | 72 h | IC50> 2500 nM | 15598814 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant PDGFRbeta (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.001μM | 27914362 | |
| Sf9 | Function assay | 1 to 4 hrs | Inhibition of recombinant human N-terminal GST/His6-tagged c-KIT (544 to 976 residues) expressed in baculovirus infected sf9 cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescen, IC50=0.001μM | 27914362 | |
| Sf9 | Function assay | 1 to 4 hrs | Inhibition of recombinant human N-terminal GST/His6-tagged FLT3 (571 to 993 residues) expressed in baculovirus infected sf9 cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescenc, IC50=0.001μM | 27914362 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant FGFR1 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.008μM | 27914362 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant VEGFR3 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.008μM | 27914362 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant VEGFR1 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.01μM | 27914362 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant VEGFR2 (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGGGQDGKDYIVLPI in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay, IC50=0.013μM | 27914362 | |
| insect cells | Function assay | 1 to 4 hrs | Inhibition of recombinant FGFR1 (unknown origin) expressed in baculovirus infected insect cells using GGGGQDGKDYIVLPI as substrate after 1 to 4 hrs by time-resolved fluorescence assay, IC50=0.008μM | 30503938 | |
| MFE319 | Growth Inhibition Assay | IC50=1.87 ± 0.45 μM | 23443805 | ||
| EN | Growth Inhibition Assay | IC50=1.66 ± 0.01 μM | 23443805 | ||
| USPC2 | Growth Inhibition Assay | IC50=1.62 ± 0.01 μM | 23443805 | ||
| SNGM | Growth Inhibition Assay | IC50=1.42 ± 0.13 μM | 23443805 | ||
| KLE | Growth Inhibition Assay | IC50=1.37 ± 0.02 μM | 23443805 | ||
| HEC1A | Growth Inhibition Assay | IC50=1.34 ± 0.30 μM | 23443805 | ||
| ISHIKAWA | Growth Inhibition Assay | IC50=1.30 ± 0.11 μM | 23443805 | ||
| SNGII | Growth Inhibition Assay | IC50=1.24 ± 0.28 μM | 23443805 | ||
| EN1 | Growth Inhibition Assay | IC50=1.02 ± 0.25 μM | 23443805 | ||
| RL952 | Growth Inhibition Assay | IC50=0.93 ± 0.01 μM | 23443805 | ||
| SPAC1S | Growth Inhibition Assay | IC50=0.77 ± 0.08 μM | 23443805 | ||
| MFE296 | Growth Inhibition Assay | IC50=0.66 ± 0.19 μM | 23443805 | ||
| HEC155 | Growth Inhibition Assay | IC50=0.66 ± 0.09 μM | 23443805 | ||
| AN3CA | Growth Inhibition Assay | IC50=0.50 ± 0.10 μM | 23443805 | ||
| MFE280 | Growth Inhibition Assay | IC50=0.42 ± 0.06 μM | 23443805 | ||
| LS174T | Growth Inhibition Assay | IC50=4.330.47 μM | 24495750 | ||
| CaCO2 | Growth Inhibition Assay | IC50=3.230.64 μM | 24495750 | ||
| SW-480 | Growth Inhibition Assay | IC50=4.330.47 μM | 24495750 | ||
| HT-29 | Growth Inhibition Assay | IC50=5.21.93 μM | 24495750 | ||
| HCT-116 | Growth Inhibition Assay | IC50=3.050.58 μM | 24495750 | ||
| RS4:11 | Growth Inhibition Assay | IC50=2.81 μM | 25202072 | ||
| HB-1119 | Growth Inhibition Assay | IC50=0.028 μM | 25202072 | ||
| SEM-K2 | Growth Inhibition Assay | IC50=0.022 μM | 25202072 | ||
| Nalm-6 | Growth Inhibition Assay | IC50=0.382 μM | 25202072 | ||
| CEM/C2 | Growth Inhibition Assay | IC50=1.125 μM | 25202072 | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.398 μM | 25202072 | ||
| BaF3-p210Bcr-Abl-T315I | Growth Inhibition Assay | IC50=2.626 μM | 25202073 | ||
| BaF3-p210Bcr-Abl | Growth Inhibition Assay | IC50=0.692 μM | 25202073 | ||
| BaF3-pSRα | Growth Inhibition Assay | IC50=0.668 μM | 25202073 | ||
| SupB15-R | Growth Inhibition Assay | IC50=0.558 μM | 25202073 | ||
| SupB15 | Growth Inhibition Assay | IC50=0.449 μM | 25202073 | ||
| EFE184 | Growth Inhibition Assay | IC50=2.04 ± 0.13 μM | 23443805 | ||
| ECC1 | Growth Inhibition Assay | IC50=2.07 ± 0.01 μM | 23443805 | ||
| HEC1B | Growth Inhibition Assay | IC50=2.57 ± 0.23 μM | 23443805 | ||
| USPC1 | Growth Inhibition Assay | IC50=2.60 ± 0.13 μM | 23443805 | ||
| SPAC1L | Growth Inhibition Assay | IC50=3.06 ± 1.14 μM | 23443805 | ||
| KM12L4A | Function assay | Inhibition of VEGFR2 phosphorylation expressed in human KM12L4A cells by Western blot analysis, EC50=0.046μM | 19113866 | ||
| KM12L4A | Function assay | Inhibition of PDGFRbeta phosphorylation expressed in human KM12L4A cells Western blot analysis, EC50=0.051μM | 19113866 | ||
| KM12L4A | Function assay | Inhibition of FGFR1 phosphorylation expressed in human KM12L4A cells by Western blot analysis, EC50=0.166μM | 19113866 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂，在无细胞试验中对III型(FLT3/c-Kit)作用最强，IC50为1 nM/2 nM，同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs，IC50为8-13 nM，但对InsR，EGFR，c-Met，EphA2，Tie2，IGF-1R和HER2作用较弱。Phase 4。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | Dovitinib是MMRC的首要候选药MMRC, 促进多发性骨髓瘤药物研究；MMRC是汇合领先学术机构的非盈利机构。 | |||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Dovitinib有效抑制FGFR1/3和VEFFR1-2，IC50为8-13 nM。Dovitinib对InsR, EGFR, c-Met, EphrinA2, Tie2, IGFR1,和HER2抑制效果不大。Dovitinib作用于FGF刺激的野生型B9细胞和F384L突变型B9细胞的生长显示出强细胞毒性，IC50为25 nM。然而，Dovitinib作用于MINV突变型B9细胞显示出低细胞毒性。Dovitinib抑制下游ERK1/2的磷酸化作用。[1] Dovitinib作用于MV4;11 (FLT-3 ITD突变型)时比作用于RS4;11 (FLT-3野生型)显示出更高的抗恶性细胞增生的能力。[2] 另一方面，Dovitinib也选择性地抑制FGFR1癌基因配体2-FGFR-阳性的KG1和KG1A细胞系，这些细胞系有FGFR1癌基因配体2-FGFR１聚合基因。另外，Dovitinib抑制8p11骨髓增殖综合征(EMS)病人的原代细胞生长。[3] |
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| 激酶实验 | 体外激酶实验 | |||
| 在体外研究时，Dovitinib溶解在DMSO中，浓度达到20mM,在实验使用前用培养基稀释。FGFR3, FGFR1, PDGFR-β, 和VEGFR1-3的激酶域在含有如下物质的混合物中测定。混合物包含50 mM HEPES (pH 7.0), 2 mM MgCl2, 10 mM MnCl2，1 mM NaF, 1 mM DTT (二硫苏糖醇), 1 mg/mL BSA (牛血清清蛋白), 0.25 µM 生物肽段基质(GGGGQDGKDYIVLPI), 1到30 µM ATP (加量取决于酶的Km值)。测定c-KIT 和FLT3的反应，调节PH到7.5，先加入0.25 到1 µM生物肽段基质(GGLFDDPSYVNVQNL)，然后加入0.2到 8 µM ATP。反应在室温下温育1到4小时，磷酸化的肽段移到含有封闭缓冲液(含25 mM EDTA和50 mM HEPES, pH 为7.5)，且包被链霉亲和素的微量滴定板上。使用回归曲线计算IC50值。 | ||||
| 细胞实验 | 细胞系 | B9细胞及多发性骨髓瘤细胞(Y373C, G384D, K650E，和J807C) | ||
| 浓度 | 400 nM 左右 | |||
| 孵育时间 | 72小时 | |||
| 方法 | MTT实验测细胞活力，B9细胞及多发性骨髓瘤细胞按5x103或20x103密度接种在96孔板上。细胞加入30 ng/mL aFGF和100 µg/mL肝素或者1% IL-6 ,及Dovitinib 温育72小时，然后测定细胞活力。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CDK1 / p-CDK1 / p53 / p21 p-PDGFR-β / PDGFR-β / p-ERK / ERK p-VEGFR-2 / VEGFR-2 / p-FGFR-1 / FGFR-1 p-STAT3 / STAT3 / Mcl-1 / LC3 / Beclin 1 / p62 |
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24238094 | |
| Growth inhibition assay | Cell viability |
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28467797 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在KMS-11移植鼠模型中，按鼠体重，每千克处理60 mg Dovitinib，导致FGFR3的衰退，结果肿瘤生长抑制率达到94%。[1] 在SCID-NOD 鼠中，Dovitinib作用于MV4;11肿瘤时显示出强的抗癌活性。[2] Dovitinib也有效抑制能激活FGFR3的KMS-11肿瘤。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 右侧腹皮下注射KMS-11细胞的雌性BNX 鼠 |
| Dosages | 10, 30,或60 mg/kg | |
| Administration | 饲喂处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05571969 | Recruiting | Advanced Solid Tumors |
Allarity Therapeutics|Amarex Clinical Research |
February 20 2023 | Phase 1 |
| NCT02268435 | Withdrawn | Gastrointestinal Stromal Tumors |
Asan Medical Center |
March 2015 | Phase 1 |
| NCT01700270 | Completed | Advanced Solid Tumors Excluding Breast Cancer |
Novartis Pharmaceuticals|Novartis |
May 2013 | Phase 1 |
| NCT01680796 | Withdrawn | Multiple Myeloma |
University of Florida|Novartis Pharmaceuticals |
February 2013 | Phase 1 |
| NCT01266070 | Terminated | Von Hippel-Lindau Syndrome |
M.D. Anderson Cancer Center|Novartis |
November 2012 | Phase 2 |
化学信息&溶解度
| 分子量 | 392.43 | 分子式 | C21H21FN6O |
| CAS号 | 405169-16-6 | SDF | Download Dovitinib (TKI-258) SDF |
| Smiles | CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 30 mg/mL ( (76.44 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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