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Vandetanib

別名: ZD6474 中文名稱：凡德他尼

Vandetanib是一種有效的 VEGFR2 抑制劑，在無細(xì)胞試驗(yàn)中IC50為40 nM。同時，也抑制VEGFR3和EGFR，IC50分別為110 nM 和500 nM。對PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50為 1.1-3.6 μM, 對MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R幾乎沒有作用效果，IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通過提高 reactive oxygen species (ROS) 的水平來誘導(dǎo)自噬。

Vandetanib Chemical Structure

Vandetanib Chemical Structure

CAS: 443913-73-3

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1570 現(xiàn)貨
25mg 1211.82 現(xiàn)貨
50mg 2104.83 現(xiàn)貨
100mg 3835.98 現(xiàn)貨
500mg 5468.77 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Vandetanib相關(guān)產(chǎn)品

相關(guān)信號通路圖

VEGFR Signaling Pathways

VEGFR信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)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?μ?? 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?μ?? 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?μ?? 6/12/24 h increases the LC3-II level in a time-dependent and dose-dependent manner 23799852
U251? Function Assay 2/4/8?μ?? 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

產(chǎn)品描述 Vandetanib是一種有效的 VEGFR2 抑制劑，在無細(xì)胞試驗(yàn)中IC50為40 nM。同時，也抑制VEGFR3和EGFR，IC50分別為110 nM 和500 nM。對PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50為 1.1-3.6 μM, 對MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R幾乎沒有作用效果，IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通過提高 reactive oxygen species (ROS) 的水平來誘導(dǎo)自噬。
靶點(diǎn)
VEGFR2 [1]
(Cell-free assay)		 VEGFR3 [1]
(Cell-free assay)		 EGFR [1]
(Cell-free assay)
40 nM 110 nM 500 nM
體外研究(In Vitro)
體外研究活性 Vandetanib 也抑制VEGFR3和EGFR，IC50分別為110 nM 和500 nM。Vandetanib 對PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50為 1.1-3.6 μM, 而對MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R幾乎沒有作用效果，IC50 > 10 μM。Vandetanib 抑制VEGF-, EGF- 和 bFGF-刺激的 HUVEC 增殖，IC50分別為60 nM, 170 nM 和 800 nM, 而對基底內(nèi)皮細(xì)胞生長幾乎沒有作用效果。Vandetanib 抑制腫瘤細(xì)胞生長，IC50 為 2.7 μM (A549) 到13.5 μM (Calu-6)。[1] Vandetanib抑制basal ABCG2-ATP酶。親本和表達(dá)ABCG2的A431細(xì)胞對 Vandetanib具有相似的敏感性。EGFR 抑制劑處理A431細(xì)胞，降低pEGFR水平，而Vandetanib 處理時，抑制效果溫和。Gefitinib, Pelitinib 和 Neratinib完全抑制 ABCG2調(diào)節(jié)的Mitoxantrone從 A431/ABCG2細(xì)胞中外排，而Vandetanib只具有微弱且不可測量的抑制效果，與 特點(diǎn)ABCG2抑制劑Ko143類似。[2] Vandetanib抑制PC3wt 和PC3R細(xì)胞系，IC50分別為13.3 μM和11.5 μM。[3] Vandetanib 作用于HUVEC，抑制VEGFR-2磷酸化,作用于肝癌細(xì)胞，抑制EGFR磷酸化，且抑制細(xì)胞增殖。[4] Vandetanib 作用于GEO 和 OVCAR-3 細(xì)胞，使細(xì)胞在G0-G1期累積，作用于OVCAR-3, ZR-75-1, MCF-10A ras, 和 GEO 細(xì)胞，促進(jìn)凋亡。Vandetanib 作用于小鼠NIH-EGFR 成纖維細(xì)胞和人類 MCF-10A ras 乳腺癌細(xì)胞（這兩種細(xì)胞都過量表達(dá)人類EGFR），抑制EGFR磷酸化，這種作用存在劑量依賴性。Vandetanib 作用于有功能性EGFR但是缺失VEGFR-2的人類細(xì)胞系 (乳腺，結(jié)腸，胃，和卵巢)，抑制軟瓊脂生長，這種作用具有劑量依賴性。[5]
激酶實(shí)驗(yàn) 激酶抑制實(shí)驗(yàn)
Vandetanib 與酶, 10 mM MnCl2, 和 2 μM ATP在聚(Glu, Ala, Tyr) 6:3:1隨機(jī)共聚物底物包被的96孔板上溫育。通過與小鼠IgG抗-磷酸酪氨酸4G10抗體，一種辣根過氧化物酶連接的羊抗鼠免疫球蛋白抗體，和2,2
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis肺癌細(xì)胞
濃度 0.1–100 μM
孵育時間 72 小時
方法

腫瘤細(xì)胞按預(yù)先制定密度接種在各自培養(yǎng)基中，確保在實(shí)驗(yàn)期間處于對數(shù)生長期 (PC-3細(xì)胞每孔500個;其他細(xì)胞每孔 1000 個)。 實(shí)驗(yàn)板在37oC下 含 CO2環(huán)境下溫育24小時，然后加入 Vandetanib (0.1–100 μM) 或空白對照 (0.1% DMSO，在培養(yǎng)基中)。實(shí)驗(yàn)板再預(yù)溫育72小時，然后使用beta 計(jì)數(shù)器通過測定 [3 H]胸甘滲透率而測評價細(xì)胞增殖。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-ERK / ERK / p-AKT / AKT p-EGFR / EGFR 19622715
Growth inhibition assay Cell viability 24261856
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Vandetanib (2.5 mg/kg, 靜脈注射)逆轉(zhuǎn) 63%VEGF誘導(dǎo)的低血壓，但是不會顯著影響bFGF誘導(dǎo)的低血壓。Vandetanib (100 mg/kg) 抑制79%腫瘤誘導(dǎo)的血管形成。Vandetanib (12.5-100 mg/kg, 口服處理) 作用于人類移植瘤，包括 Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis 肺癌，顯著抑制腫瘤生長，而對體重幾乎沒有影響。[1] Vandetanib單獨(dú)作用于PC3wt移植瘤，施加似是而非的腫瘤生長刺激作用。Vandetanib按25 mg/kg低劑量處理PC3R移植瘤，與對照組相比，明顯顯著效果，而按50 mg/kg高劑量處理，與對照組相比，則顯著抑制腫瘤生長。相反, Vandetanib 50 mg/kg 和Docetaxel 30 mg/kg 按高劑量聯(lián)用作用于PC3R細(xì)胞，卻具有顯著的負(fù)相互作用。[3]Vandetanib 作用于攜帶腫瘤的小鼠，抑制腫瘤組織中的VEGFR-2 和EGFR磷酸化，顯著降低腫瘤血管密度，增強(qiáng)腫瘤細(xì)胞凋亡,抑制腫瘤生長，促進(jìn)生存,降低肝內(nèi)轉(zhuǎn)移數(shù)量,且上調(diào)腫瘤組織中的VEGF, TGF-alpha和EGF。Vandetanib處理與嚴(yán)重不良事件，包括ALT異常，骨髓抑制或體重減輕無關(guān)。[4]Vandetanib 作用于攜帶GEO結(jié)腸癌移植瘤(對EGFR 信號受抑制敏感)的裸鼠，抑制腫瘤生長，這種作用存在劑量依賴性。[5]
動物實(shí)驗(yàn) Animal Models 攜帶 PC-3, Calu-6, SKOV-3, 和 MDA-MB-231腫瘤的雌性無胸腺(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 口服處理
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

化學(xué)信息&溶解度

分子量 475.35 分子式

C22H24BrFN4O2
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 60 mg/mL ( (126.22 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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