Vandetanib
别名: ZD6474 中文名称：凡德他尼
Vandetanib是一种有效的 VEGFR2 抑制剂，在无细胞试验中IC50为40 nM。同时，也抑制VEGFR3和EGFR，IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果，IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通过提高 reactive oxygen species (ROS) 的水平来诱导自噬。
Vandetanib Chemical Structure
CAS: 443913-73-3
产品质控
批次：
纯度：
99.99%
99.99
Vandetanib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 |
|---|---|---|---|---|---|
| PCI-15B | Function Assay | 1 μM | 24 h | downregulates VEGF production | 22307735 |
| UM-22A | Function Assay | 1 μM | 24 h | downregulates VEGF production | 22307735 |
| PCI-37A | Function Assay | 1 μM | 24 h | downregulates VEGF production | 22307735 |
| PCI-15B | Function Assay | 0-10 μM | 24 h | inhibits the activation of the EGFR tyrosine kinase and also decreases the expression of phosphorylated forms of the downstream signaling elements, STAT3 and MAPK | 22307735 |
| UM-22B | Function Assay | 0-10 μM | 24 h | inhibits the activation of the EGFR tyrosine kinase and also decreases the expression of phosphorylated forms of the downstream signaling elements, STAT3 and MAPK | 22307735 |
| UM-22A | Function Assay | 0-10 μM | 24 h | inhibits the activation of the EGFR tyrosine kinase and also decreases the expression of phosphorylated forms of the downstream signaling elements, STAT3 and MAPK | 22307735 |
| SCC-25 | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| PCI-15B | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| PCI-37B | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| PCI-37A | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| UM-22B | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| UM-22A | Growth Inhibition Assay | 0-6 μM | 72 h | inhibits cell growth in a dose dependent manner | 22307735 |
| HAK1-B | Function Assay | 1/5/10 μM | 1 h | suppresses EGFR phosphorylation | 22611027 |
| HUVECs | Function Assay | 1/5/10 μM | 1 h | significantly inhibits VEGFR-2 phosphorylation | 22611027 |
| U87MG | Function Assay | 4 μℳ | 2/6/12 h | suppresses basal levels of phosphorylation of S6 (S235/236), 4E-BP1 (T37/46), and Akt (S473) in a time-dependent manner | 23799852 |
| U251 | Function Assay | 4 μℳ | 2/6/12 h | suppresses basal levels of phosphorylation of S6 (S235/236), 4E-BP1 (T37/46), and Akt (S473) in a time-dependent manner | 23799852 |
| U87MG | Function Assay | 2/4/8 μℳ | 6/12/24 h | increases the LC3-II level in a time-dependent and dose-dependent manner | 23799852 |
| U251 | Function Assay | 2/4/8 μℳ | 6/12/24 h | increases the LC3-II level in a time-dependent and dose-dependent manner | 23799852 |
| MDA-MB-468 | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| T-47-D | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| MDA-MB-231 | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| ZR-75-1 | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| MCF-7 | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| HMEpC | Growth Inhibition Assay | 1 nM-100 μM | 48 h | inhibits cell growth in a dose dependent manner | 24138843 |
| SH-SY5Y | Function Assay | 5 μM | 48/72 h | suppresses expression of the CXCR4 and MMP14 protein | 24399074 |
| SK-N-SH | Function Assay | 5 μM | 48/72 h | suppresses expression of the CXCR4 and MMP14 protein | 24399074 |
| SH-SY5Y | Function Assay | 5 μM | 24/48/72 h | suppresses the expression of CXCR4 and MMP14 mRNA | 24399074 |
| SK-N-SH | Function Assay | 5 μM | 24/48/72 h | suppresses the expression of CXCR4 and MMP14 mRNA | 24399074 |
| SH-SY5Y | Function Assay | 5/10 μM | 48 h | inhibits human NB cell invasion | 24399074 |
| SK-N-SH | Function Assay | 5/10 μM | 48 h | inhibits human NB cell invasion | 24399074 |
| SH-SY5Y | Function Assay | 5/10 μM | 48 h | inhibits human NB cell migration | 24399074 |
| SK-N-SH | Function Assay | 5/10 μM | 48 h | inhibits human NB cell migration | 24399074 |
| SH-SY5Y | Function Assay | 1/5/10 μM | 48 h | inhibits RET phosphorylation | 24399074 |
| SK-N-SH | Function Assay | 1/5/10 μM | 48 h | inhibits RET phosphorylation | 24399074 |
| SH-SY5Y | Function Assay | 5/10/20 μM | 48 h | induces G1 phase cell cycle arrest | 24399074 |
| SK-N-SH | Function Assay | 5/10/20 μM | 48 h | induces G1 phase cell cycle arrest | 24399074 |
| SH-SY5Y | Apoptosisi Assay | 5/10/20 μM | 48 h | induces apoptosis dose dependently | 24399074 |
| SK-N-SH | Apoptosisi Assay | 5/10/20 μM | 48 h | induces apoptosis dose dependently | 24399074 |
| SH-SY5Y | Growth Inhibition Assay | 0.625-20 μM | 48 h | inhibits cell growth in a dose dependent manner | 24399074 |
| SK-N-SH | Growth Inhibition Assay | 0.625-20 μM | 48 h | inhibits cell growth in a dose dependent manner | 24399074 |
| SN179 | Function Assay | 500 nM | 16 h | increases basal migration | 25676691 |
| SN179 | Function Assay | 500 nM | 16 h | enhances the CXCL12 directed migration | 25676691 |
| SN186 | Function Assay | 500 nM | 16 h | increases CXCR4 expression significantly | 25676691 |
| SN179 | Function Assay | 500 nM | 16 h | increases CXCR4 expression significantly | 25676691 |
| 201T | Function Assay | 2.5 μM | 48 h | inhibits phospho-MAPK following EGF | 22258476 |
| 273T | Function Assay | 2.5 μM | 48 h | inhibits phospho-MAPK following EGF | 22258476 |
| A549 | Function Assay | 2.5 μM | 48 h | inhibits phospho-MAPK following EGF | 22258476 |
| 201T | Function Assay | 1/5/10 μM | 48 h | blocks the phosphorylation of Akt induced by VEGFC | 22258476 |
| HTB3 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| HT1376 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| RT4 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| J82 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| CRL1749 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| T24 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| SUP | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| HTB9 | Growth Inhibition Assay | 0-20 μM | 24 h | inhibits cell growth in a dose dependent manner | 19220256 |
| ACC3 | Growth Inhibition Assay | 0-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 18698025 |
| ACC2 | Growth Inhibition Assay | 0-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 18698025 |
| ACCM | Growth Inhibition Assay | 0-10 μM | 72 h | inhibits cell growth in a dose dependent manner | 18698025 |
| ACC3 | Apoptosisi Assay | 0-10 μM | 72 h | induces apoptosis dose dependently | 18698025 |
| ACC2 | Apoptosisi Assay | 0-10 μM | 72 h | induces apoptosis dose dependently | 18698025 |
| ACCM | Apoptosisi Assay | 0-10 μM | 72 h | induces apoptosis dose dependently | 18698025 |
| CNE-1 | Growth Inhibition Assay | 0.1-25.6 μM | 48 h | IC50=3.6 μM | 17631646 |
| CNE-2 | Growth Inhibition Assay | 0.1-25.6 μM | 48 h | IC50=6.2 μM | 17631646 |
| C666-1 | Growth Inhibition Assay | 0.1-25.6 μM | 48 h | IC50=23.4 μM | 17631646 |
| CNE-1 | Growth Inhibition Assay | 0.1-25.6 μM | 72 h | IC50=2.3 μM | 17631646 |
| CNE-2 | Growth Inhibition Assay | 0.1-25.6 μM | 72 h | IC50=3.6 μM | 17631646 |
| C666-1 | Growth Inhibition Assay | 0.1-25.6 μM | 72 h | IC50=4.86 μM | 17631646 |
| CNE-1 | Function Assay | 6 μM | 24 h | delays G0/G1 cell cycle progression | 17631646 |
| CNE-2 | Function Assay | 6 μM | 24 h | delays G0/G1 cell cycle progression | 17631646 |
| C666-1 | Function Assay | 6 μM | 24 h | delays G0/G1 cell cycle progression | 17631646 |
| HT-29 | Antiproliferative assay | 10 uM | 72 hrs | Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MTS assay, IC50 = 4.2 μM. | 21353546 |
| EAhy926 | Antiproliferative assay | 10 uM | 72 hrs | Antiproliferative activity against human EAhy926 cells at 10 uM after 72 hrs by MTS assay, IC50 = 5.1 μM. | 21353546 |
| SCC-25 | Invasion Assay | 24 h | EC50=10 nM | 22307735 | |
| UM-22A | Invasion Assay | 24 h | EC50=0.3 nM | 22307735 | |
| PCI-37A | Invasion Assay | 24 h | EC50=1695 nM | 22307735 | |
| PCI-15B | Invasion Assay | 24 h | EC50=558 nM | 22307735 | |
| HuH-7 | Growth Inhibition Assay | 72 h | IC50 = 9.4 μmol/L | 22611027 | |
| KYN-2 | Growth Inhibition Assay | 72 h | IC50 = 8.1 μmol/L | 22611027 | |
| HUVECs | Growth Inhibition Assay | 72 h | IC50 = 7.1 μmol/L | 22611027 | |
| A-431 | Growth Inhibition Assay | 72 h | GI50=2.4 ± 0.3 μM | 24681205 | |
| NCTC-2544 | Growth Inhibition Assay | 72 h | GI50=4.6 ± 0.3 μM | 24681205 | |
| K-562 | Growth Inhibition Assay | 72 h | GI50=1.8 ± 0.1 μM | 24681205 | |
| Jurkat | Growth Inhibition Assay | 72 h | GI50=1.5 ± 0.2 μM | 24681205 | |
| UM-22B | Invasion Assay | 24 h | EC50=2424 nM | 22307735 | |
| PCI-37B | Invasion Assay | 24 h | EC50=1726 nM | 22307735 | |
| Hth83 | Growth Inhibition Assay | 72 h | IC50=3.30 ± 0.66 μM | 21220477 | |
| C643 | Growth Inhibition Assay | 72 h | IC50=3.65 ± 1.22 μM | 21220477 | |
| 8505C | Growth Inhibition Assay | 72 h | IC50=7.56 ± 1.13 μM | 21220477 | |
| Hth74 | Growth Inhibition Assay | 72 h | IC50=8.56 ± 1.01 μM | 21220477 | |
| SW1736 | Growth Inhibition Assay | 72 h | IC50=9.05 ± 0.55 μM | 21220477 | |
| Hth7 | Growth Inhibition Assay | 72 h | IC50=9.66 ± 0.38 μM | 21220477 | |
| Hth104 | Growth Inhibition Assay | 72 h | IC50=±16.98 ± NA μM | 21220477 | |
| EHMES-1 | Growth Inhibition Assay | 72 h | IC50=10.6 μM | 18364248 | |
| EHMES-10 | Growth Inhibition Assay | 72 h | IC50=0.3 μM | 18364248 | |
| 211H | Growth Inhibition Assay | 72 h | IC50=2.2 μM | 18364248 | |
| H28 | Growth Inhibition Assay | 72 h | IC50=1.8 μM | 18364248 | |
| H2052 | Growth Inhibition Assay | 72 h | IC50=8.0 μM | 18364248 | |
| H2452 | Growth Inhibition Assay | 72 h | IC50=5.5 μM | 18364248 | |
| TPC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human TPC1 cells expressing RET/PCT1 after 72 hrs by [3H]thymidine incorporation assay, IC50 = 0.116 μM. | 20409618 | |
| Sf21 | Function assay | 15 mins | Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay, IC50 = 0.175 μM. | 26874741 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.4 μM. | 26874741 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.63 μM. | 26874741 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50 = 1.492 μM. | 26995527 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 1.925 μM. | 26995527 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay, IC50 = 1.974 μM. | 26995527 | |
| MGHU3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay, IC50 = 2.5 μM. | 30309671 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay, IC50 = 2.5 μM. | 30309671 | |
| RT112 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay, IC50 = 2.5 μM. | 30309671 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 2.63 μM. | 26995527 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 3.536 μM. | 26995527 | |
| PANC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay, IC50 = 4.107 μM. | 26995527 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay, IC50 = 11.83 μM. | 27688180 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50 = 16.52 μM. | 28942113 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 18.5 μM. | 26741358 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 18.5 μM. | 26475519 | |
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells measured after 48 hrs by MTT assay, IC50 = 18.95 μM. | 27688180 | |
| H460 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human H460 cells measured after 48 hrs by MTT assay, IC50 = 37.1 μM. | 27688180 | |
| H1650 | Growth Inhibition Assay | IC50=3.5±1.2 μM | 23274758 | ||
| H2052 | Growth Inhibition Assay | IC50=1.07±0.04 μM | 21970874 | ||
| H2452 | Growth Inhibition Assay | IC50=3.52±1.13 μM | 21970874 | ||
| H28 | Growth Inhibition Assay | IC50=0.32±0.07 μM | 21970874 | ||
| MSTO-211H | Growth Inhibition Assay | IC50=1.42±0.03 μM | 21970874 | ||
| KDR15 | Function assay | Inhibitory activity against VEGF stimulated autophosphorylation of VEGFR2 expressed in KDR15 cells, IC50 = 0.015 μM. | 16302797 | ||
| Sf9 | Function assay | Inhibition of human recombinant histidine-tagged RET (700-1020) expressed in Sf9 cells by ELISA, IC50 = 0.097 μM. | 20409618 | ||
| HEK293 | Function assay | Inhibition of FGFR1/VEGFR2 chimeric construct expressed in HEK293 cells by ELISA, ED50 = 0.15 μM. | 19101155 | ||
| umbilical vein endothelial cells | Function assay | Inhibition of VEGF-induced proliferation of human umbilical vein endothelial cells, IC50 = 0.4 μM. | 15743202 | ||
| umbilical vein endothelial cells | Function assay | Inhibition of basic FGF-induced proliferation of human umbilical vein endothelial cells, IC50 = 1.2 μM. | 15743202 | ||
| 293 | Function assay | Inhibitory activity against VEGFR2 transiently transfected in 293 adenovirus transfected kidney cells by ELISA, IC50 = 1.66 μM. | 16275072 | ||
| 293 | Function assay | Inhibition of VEGFR2 in 293 adenovirus transfected kidney cells by cell-based ELISA assay, IC50 = 1.66 μM. | 16321531 | ||
| HEK293 | Function assay | Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA, IC50 = 1.66 μM. | 16460936 | ||
| CHO | Function assay | Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells, IC50 = 2.673 μM. | 12477352 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Vandetanib是一种有效的 VEGFR2 抑制剂，在无细胞试验中IC50为40 nM。同时，也抑制VEGFR3和EGFR，IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果，IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通过提高 reactive oxygen species (ROS) 的水平来诱导自噬。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Vandetanib 也抑制VEGFR3和EGFR，IC50分别为110 nM 和500 nM。Vandetanib 对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50为 1.1-3.6 μM, 而对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果，IC50 > 10 μM。Vandetanib 抑制VEGF-, EGF- 和 bFGF-刺激的 HUVEC 增殖，IC50分别为60 nM, 170 nM 和 800 nM, 而对基底内皮细胞生长几乎没有作用效果。Vandetanib 抑制肿瘤细胞生长，IC50 为 2.7 μM (A549) 到13.5 μM (Calu-6)。[1] Vandetanib抑制basal ABCG2-ATP酶。亲本和表达ABCG2的A431细胞对 Vandetanib具有相似的敏感性。EGFR 抑制剂处理A431细胞，降低pEGFR水平，而Vandetanib 处理时，抑制效果温和。Gefitinib, Pelitinib 和 Neratinib完全抑制 ABCG2调节的Mitoxantrone从 A431/ABCG2细胞中外排，而Vandetanib只具有微弱且不可测量的抑制效果，与 特点ABCG2抑制剂Ko143类似。[2] Vandetanib抑制PC3wt 和PC3R细胞系，IC50分别为13.3 μM和11.5 μM。[3] Vandetanib 作用于HUVEC，抑制VEGFR-2磷酸化,作用于肝癌细胞，抑制EGFR磷酸化，且抑制细胞增殖。[4] Vandetanib 作用于GEO 和 OVCAR-3 细胞，使细胞在G0-G1期累积，作用于OVCAR-3, ZR-75-1, MCF-10A ras, 和 GEO 细胞，促进凋亡。Vandetanib 作用于小鼠NIH-EGFR 成纤维细胞和人类 MCF-10A ras 乳腺癌细胞（这两种细胞都过量表达人类EGFR），抑制EGFR磷酸化，这种作用存在剂量依赖性。Vandetanib 作用于有功能性EGFR但是缺失VEGFR-2的人类细胞系 (乳腺，结肠，胃，和卵巢)，抑制软琼脂生长，这种作用具有剂量依赖性。[5] | |||
|---|---|---|---|---|
| 激酶实验 | 激酶抑制实验 | |||
| Vandetanib 与酶, 10 mM MnCl2, 和 2 μM ATP在聚(Glu, Ala, Tyr) 6:3:1随机共聚物底物包被的96孔板上温育。通过与小鼠IgG抗-磷酸酪氨酸4G10抗体，一种辣根过氧化物酶连接的羊抗鼠免疫球蛋白抗体，和2,2 | ||||
| 细胞实验 | 细胞系 | Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis肺癌细胞 | ||
| 浓度 | 0.1–100 μM | |||
| 孵育时间 | 72 小时 | |||
| 方法 | 肿瘤细胞按预先制定密度接种在各自培养基中，确保在实验期间处于对数生长期 (PC-3细胞每孔500个;其他细胞每孔 1000 个)。 实验板在37oC下 含 CO2环境下温育24小时，然后加入 Vandetanib (0.1–100 μM) 或空白对照 (0.1% DMSO，在培养基中)。实验板再预温育72小时，然后使用beta 计数器通过测定 [3 H]胸甘渗透率而测评价细胞增殖。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-ERK / ERK / p-AKT / AKT p-EGFR / EGFR |
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19622715 | |
| Growth inhibition assay | Cell viability |
|
24261856 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Vandetanib (2.5 mg/kg, 静脉注射)逆转 63%VEGF诱导的低血压，但是不会显著影响bFGF诱导的低血压。Vandetanib (100 mg/kg) 抑制79%肿瘤诱导的血管形成。Vandetanib (12.5-100 mg/kg, 口服处理) 作用于人类移植瘤，包括 Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis 肺癌，显著抑制肿瘤生长，而对体重几乎没有影响。[1] Vandetanib单独作用于PC3wt移植瘤，施加似是而非的肿瘤生长刺激作用。Vandetanib按25 mg/kg低剂量处理PC3R移植瘤，与对照组相比，明显显著效果，而按50 mg/kg高剂量处理，与对照组相比，则显著抑制肿瘤生长。相反, Vandetanib 50 mg/kg 和Docetaxel 30 mg/kg 按高剂量联用作用于PC3R细胞，却具有显著的负相互作用。[3]Vandetanib 作用于携带肿瘤的小鼠，抑制肿瘤组织中的VEGFR-2 和EGFR磷酸化，显著降低肿瘤血管密度，增强肿瘤细胞凋亡,抑制肿瘤生长，促进生存,降低肝内转移数量,且上调肿瘤组织中的VEGF, TGF-alpha和EGF。Vandetanib处理与严重不良事件，包括ALT异常，骨髓抑制或体重减轻无关。[4]Vandetanib 作用于携带GEO结肠癌移植瘤(对EGFR 信号受抑制敏感)的裸鼠，抑制肿瘤生长，这种作用存在剂量依赖性。[5] | |
|---|---|---|
| 动物实验 | Animal Models | 携带 PC-3, Calu-6, SKOV-3, 和 MDA-MB-231肿瘤的雌性无胸腺(nu/nu 基因型) Swiss小鼠 |
| Dosages | 12.5 mg/kg/day, 25 mg/kg/day, 50 mg/kg/day, 或 100 mg/kg/day | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03291379 | Completed | Carcinoma Hepatocellular|Metastatic Colorectal Cancer |
Boston Scientific Corporation|Biocompatibles UK Ltd |
May 17 2017 | Early Phase 1 |
| NCT02495103 | Terminated | Renal Cell Carcinoma|Hereditary Leiomyomatosis|Renal Cell Cancer |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
August 26 2015 | Phase 1|Phase 2 |
| NCT02530411 | Unknown status | Neoplasms |
Velindre NHS Trust|Cancer Research UK|AstraZeneca |
April 2015 | Phase 2 |
| NCT02268734 | Completed | Metastatic Sporadic Medullary Thyroid Cancer |
Fondazione IRCCS Istituto Nazionale dei Tumori Milano |
April 2014 | -- |
| NCT01876784 | Completed | Differentiated Thyroid Cancer |
Genzyme a Sanofi Company|Sanofi |
September 17 2013 | Phase 3 |
| NCT01661179 | Completed | Unresectable Locally Advanced or Metastatic Medullary Thyroid Carcinoma |
Genzyme a Sanofi Company|Sanofi |
November 2012 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 475.35 | 分子式 | C22H24BrFN4O2 |
| CAS号 | 443913-73-3 | SDF | Download Vandetanib SDF |
| Smiles | CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 60 mg/mL ( (126.22 mM) Warmed with 50°C water bath; Ultrasonicated; ；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 |
|
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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