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VEGFR3EGFR,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

Vandetanib Chemical Structure

CAS: 443913-73-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1096.56 现货
25mg RMB 1211.82 现货
50mg RMB 2104.83 现货
100mg RMB 3835.98 现货
500mg RMB 5468.77 现货
1g RMB 7944.3 现货
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info@selleck.cn

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客户使用Selleck的Vandetanib发表文献106

产品质控

批次: 纯度: 99.99%
99.96

Vandetanib相关产品

相关信号通路图

VEGFR抑制剂选择性比较

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
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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VEGFR3EGFR,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
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
40 nM 110 nM 500 nM
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。

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 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
批次:

DMSO : 24 mg/mL ( 50.48 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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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