Vandetanib (ZD6474)

目录号:S1046

Vandetanib (ZD6474) Chemical Structure

Molecular Weight(MW): 475.35

Vandetanib (ZD6474)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。

规格 价格 库存 购买数量  
RMB 1211.82 现货
RMB 3835.98 现货
RMB 5468.77 现货
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客户使用该产品的7个实验数据:

  • (A) Representative in vivo bioluminescence of mice at and during time of treatment. Derived cell lines with either BCR-ABL1 WT or V299L was tail-vein injected into immunocompetent recipient mice. Initial imaging was performed at day 10 post-transplantation. Mice were subsequently treated once daily with vehicle, 10 mg/kg dasatinib, 50 mg/kg imatinib, 50 mg/kg vandetanib, or 50 mg/kg foretinib.
    (B) Fold change in total whole-mouse bioluminescence signal between post- and pre-treatment. Mice bearing BCR-ABL1 V299L ALLs showed significant tumor burden reduction upon treatment with foretinib or vandetanib. Statistical significance determined by Mann-Whitney test. *p < 0.05, **p < 0.01.

    Cell, 2016, 165(1):234-46.. Vandetanib (ZD6474) purchased from Selleck.

    Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (*P0.0003). VEGF was used a positive control and increased nitrite levels (**P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels.

    Hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

  • Vandetanib reduced phosphorylation of Akt in endothelial cells (ECs). MS1 ECs were incubated with 1 μmol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]; 1 hour). Western blotting analysis showed that vandetanib decreased phosphorylation of Akt (S473) in MS1 ECs (*P<0.01; n=6 per group, studies done in triplicate). These findings show that vandetanib reduced Akt activity.

    Hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

    Vandetanib increases membrane localization of endothelial NO synthase (eNOS). MS1 endothelial cells (ECs) were incubated with 1 μmol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]). Western blotting analysis showed that vandetanib increases membrane localization of eNOS compared with control (*P<0.04; n=4 per group, studies done in triplicate). These findings show that vandetanib increased the membrane localization of eNOS compared with control.

    Hypertension 2011 58, 85-92. Vandetanib (ZD6474) purchased from Selleck.

  • (H) Anti-pSTAT3Y705, total STAT3, pSRCy416 of RWPE-1 transfectants treated for 6 hours with vandetanib at the indicated concentrations. Actin was used as loading control.

    J Cancer, 2017, 8(1):140-145. Vandetanib (ZD6474) purchased from Selleck.

    LS-007 inhibits CDK1/CDK7/CDK9 activity in AL cells. HL-60 (A), CCRF-CEM (B) cells were treated with increasing concentrations of LS-007 or flavopiridol for 2 h, and cell lysates were collected and examined by immunoblotting with the indicated antibodies.

    Acta Pharmacol Sin, 2016, 37(11):1481-1489. Vandetanib (ZD6474) purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Vandetanib for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Vandetanib (ZD6474) purchased from Selleck.

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Vandetanib (ZD6474)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。
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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SN179  MVnGeY5kfGmxbjDBd5NigQ>? M3TsTlUxOOLCiX7NxsA> NHjxXlEyPiCq MWjpcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 Mn\qNlU3PzZ4OUG=
SN186 Mk\iSpVv[3Srb36gRZN{[Xl? MWi1NFDjiImwTdMg MnfoNVYhcA>? MUHpcoNz\WG|ZYOgR3hEWjRiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 Mln1NlU3PzZ4OUG=
SN179  NV7HN4R2TnWwY4Tpc44hSXO|YYm= NWrLWIRjPTBy4pEJcm3DqA>? MX[xOkBp NULhVHVp\W6qYX7j[ZMhfGinIFPYR2wyOiCmaYLlZ5Rm\CCvaXfyZZRqd25? NV7zcoE3OjV4N{[2PVE>
SN179  NGjUdmFHfW6ldHnvckBCe3OjeR?= M{HwS|UxOOLCiX7NxsA> NV\oUY9VOTZiaB?= NFjh[3pqdmO{ZXHz[ZMh[mG|YXygcYloemG2aX;uxsA> M3fvU|I2Pjd4Nkmx
Jurkat NGHqVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTkO|LDqGkEoB?= MoKyS2k2OD1zLkWgxtEhOC5{IN88US=> M4exdVI1PjhzMkC1
K-562 MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WzR|czyqCqwrC= NH65[JlIUTVyPUGuPEDDuSByLkGg{txO MXOyOFY5OTJyNR?=
NCTC-2544 M2fiXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\hO|LDqGkEoB?= M13FRmdKPTB;ND62JOKyKDBwMzFOwG0> MX2yOFY5OTJyNR?=
A-431 M3vMVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[3NuKhcMLi MVrHTVUxRTJwNDFCtUAxNjNizszN NF6wZmEzPDZ6MUKwOS=>
SK-N-SH NIH6ZXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO2b3QxNjZ{NT2yNEDPxE1? M37zZVQ5KGh? MlLPSG1UVw>? MlLkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1P4d|I1Ozl7MEe0
SH-SY5Y M4T3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfLVZYxNjZ{NT2yNEDPxE1? NUK4UJh1PDhiaB?= NUX3N2U{TE2VTx?= MlXzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MnTxNlQ{QTlyN{S=
SK-N-SH Mk\0RZBweHSxc3nzbUBCe3OjeR?= M1PZZlUwOTBxMkCg{txO MUe0PEBp NXvsW41pTE2VTx?= MYDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M{jZWVI1Ozl7MEe0
SH-SY5Y M4LNXGFxd3C2b4Ppd4khSXO|YYm= NXjiTWlJPS9zMD:yNEDPxE1? MVu0PEBp M1jxdmROW09? M2DRR4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3;wNFI1Ozl7MEe0
SK-N-SH MkDtSpVv[3Srb36gRZN{[Xl? NWPaS2FvPS9zMD:yNEDPxE1? MmqzOFghcA>? NInZNYtFVVOR MXfpcoR2[2W|IFexJJBp[XOnIHPlcIwh[3mlbHWgZZJz\XO2 NWC4VnBNOjR|OUmwO|Q>
SH-SY5Y NXLj[HlrTnWwY4Tpc44hSXO|YYm= NYHvZ2hPPS9zMD:yNEDPxE1? NUexVppvPDhiaB?= MmnISG1UVw>? MojubY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dB?= MXyyOFM6QTB5NB?=
SK-N-SH NGHTbXJHfW6ldHnvckBCe3OjeR?= MnW2NU82NzFyIN88US=> M3TD[VQ5KGh? MnjBSG1UVw>? MV\pcohq[mm2czDSSXQheGixc4Doc5J6dGG2aX;u NF;MdnczPDN7OUC3OC=>
SH-SY5Y NHi2TohHfW6ldHnvckBCe3OjeR?= M{[0bFEwPS9zMDFOwG0> MXm0PEBp MleySG1UVw>? MXTpcohq[mm2czDSSXQheGixc4Doc5J6dGG2aX;u Mn\NNlQ{QTlyN{S=
SK-N-SH NUfje45LTnWwY4Tpc44hSXO|YYm= NWG4fos1PS9zMDFOwG0> MYG0PEBp NHvnRYVFVVOR NIDXeXRqdmirYnn0d{BpfW2jbjDORkBk\WyuIH3p[5JifGmxbh?= Moi1NlQ{QTlyN{S=
SH-SY5Y NI\QOZVHfW6ldHnvckBCe3OjeR?= NWjFeXNTPS9zMDFOwG0> NYDze5Z4PDhiaB?= M1z4VGROW09? M{\MRYlvcGmkaYTzJIh2dWGwIF7CJINmdGxibXnndoF1cW:w MXKyOFM6QTB5NB?=
SK-N-SH NIXIPI5HfW6ldHnvckBCe3OjeR?= MYS1M|ExKM7:TR?= NEHDfFc1QCCq M2jJ[WROW09? NIDMRWpqdmirYnn0d{BpfW2jbjDORkBk\WyuIHnueoF{cW:w MV2yOFM6QTB5NB?=
SH-SY5Y MUPGeY5kfGmxbjDBd5NigQ>? MXG1M|ExKM7:TR?= NFjyUlI1QCCq MlXDSG1UVw>? MYDpcohq[mm2czDoeY1idiCQQjDj[YxtKGmwdnHzbY9v MnvFNlQ{QTlyN{S=
SK-N-SH NIDVSGtHfW6ldHnvckBCe3OjeR?= NEi5SVM2KM7:TR?= MlnQNlQwPDhxN{KgbC=> NV7aclJsTE2VTx?= MmHDd5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBEYEOUNDDhcoQhVU2SMUSgcXJPSQ>? NVzKVHhFOjR|OUmwO|Q>
SH-SY5Y NUD6PWNTTnWwY4Tpc44hSXO|YYm= MWC1JO69VQ>? NEizWlMzPC92OD:3NkBp MmnJSG1UVw>? MkLId5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBEYEOUNDDhcoQhVU2SMUSgcXJPSQ>? M1zU[lI1Ozl7MEe0
SK-N-SH NIfiOHBHfW6ldHnvckBCe3OjeR?= MlHnOUDPxE1? NIjyflY1QC95MjDo NHjsTYtFVVOR MlOzd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBEYEOUNDDhcoQhVU2SMUSgdJJwfGWrbh?= NVzkd3dHOjR|OUmwO|Q>
SH-SY5Y NIf5WWpHfW6ldHnvckBCe3OjeR?= MkLkOUDPxE1? M4TtfFQ5Nzd{IHi= MVnEUXNQ M1\BVpN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhS1iFUkSgZY5lKE2PUEG0JJBzd3SnaX6= M4L1clI1Ozl7MEe0
HMEpC MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jzTlEhdk1vMUCwJO69VQ>? M{Tvd|Q5yqCqwrC= MXfEUXNQ M3XncYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NH\ZUpQzPDF|OEi0Ny=>
MCF-7 NF20bJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXCXJIyKG6PLUGwNEDPxE1? M{S1UFQ5yqCqwrC= NGT1WWNFVVOR NV;1Xmh3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXGyOFE{QDh2Mx?=
ZR-75-1 NVjCTop6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTRT2hJOSCwTT2xNFAh|ryP MUm0POKhcMLi NF3sdphFVVOR Mof1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXKyOFE{QDh2Mx?=
MDA-MB-231 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TPZVEhdk1vMUCwJO69VQ>? MVi0POKhcMLi NIi5fY9FVVOR M3PBdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4rSdlI1OTN6OESz
MDA-MB-468 M4XwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljPNUBvVS1zMECg{txO NHPae2I1QMLiaNMg MmjOSG1UVw>? MkjBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MYeyOFE{QDh2Mx?=
T-47-D MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjueJEyKG6PLUGwNEDPxE1? MWS0POKhcMLi MUfEUXNQ MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NI\WNJgzPDF|OEi0Ny=>
U251  MnruSpVv[3Srb36gRZN{[Xl? NIDqZVczNzRxOPMAje696oT|wrC= NV\We|N7Pi9zMj:yOEBp NV\vcnNxTE2VTx?= M4\BUolv[3KnYYPld{B1cGViTFOzMWlKKGyndnXsJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4DKcVI{Pzl7OEWy
U87MG NVvwbJNTTnWwY4Tpc44hSXO|YYm= NXnUfHlrOi92L{lihKnPxOLGs9Mg MVe2M|EzNzJ2IHi= MXrEUXNQ NEHC[VlqdmO{ZXHz[ZMhfGinIFzDN{1KUSCuZY\lcEBqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MViyN|c6QTh3Mh?=
U251  NXPmSZp1TnWwY4Tpc44hSXO|YYm= M3z6XVTjiIoQvPMEt:Kh NEHLdVIzNzZxMUKgbC=> M2LYNGROW09? MnLNd5VxeHKnc4Pld{Bj[XOjbDDs[ZZmdHNib3[gdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KCiVMkO1M|I{PiluIETFMWJROSBqVEO3M|Q3MSxiYX7kJGFsfCBqU{S3N{khcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NXLSbWFtOjN5OUm4OVI>
U87MG M1OwNWZ2dmO2aX;uJGF{e2G7 NHLnUms16oDLzs|iiNPDqA>? NHzSN3gzNzZxMUKgbC=> M2THTmROW09? NXf2ZYdIe3WycILld5NmeyCkYYPhcEBt\X[nbIOgc4YheGixc4Doc5J6dGG2aX;uJI9nKFN4IDjTNlM2NzJ|NjmsJFRGNUKSMTCoWFM4NzR4KTygZY5lKEGtdDCoV|Q4OyliaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?= NXzjfZk3OjN5OUm4OVI>
H1650  M2TZb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTNwNdMxNU4zKM7:TR?= M2TX[VI{Ojd2N{W4
HUVECs  NFXmbG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXsO|IhcA>? MVvJR|UxyqB;IEeuNUDPxG2xbD;M NUjTT|VROjJ4MUGwNlc>
KYN-2  M1jtXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm3NkBp NYS4SJc2UUN3MNMgQUA5NjFizsztc4wwVA>? NV\GbJpYOjJ4MUGwNlc>
HuH-7  NUDvcmMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFOyOXU4OiCq NVjGbnY{UUN3MNMgQUA6NjRizsztc4wwVA>? NWXPSpY5OjJ4MUGwNlc>
HUVECs  MYnGeY5kfGmxbjDBd5NigQ>? NV7vU29MOS93L{GwJO69VQ>? NV;x[XNLOSCq M3:wVpNq\26rZnnjZY51dHliaX7obYJqfHNiVlXHSnIuOiCyaH;zdIhwenmuYYTpc44> MVWyNlYyOTB{Nx?=
HAK1-B NILYfldHfW6ldHnvckBCe3OjeR?= NYP5Om1{OS93L{GwJO69VQ>? NWHYTmVHOSCq MnzWd5VxeHKnc4Pld{BGT0[UIIDoc5NxcG:{eXzheIlwdg>? MWKyNlYyOTB{Nx?=
UM-22A NX[ybXdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVntWJg6OC14IN88US=> M2PVUVczKGh? MXPEUXNQ MmT0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NVPx[4I4OjJ|MEe3N|U>
UM-22B M4f4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKwMVYh|ryP MnnEO|IhcA>? MYXEUXNQ M1TTUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4i2XVIzOzB5N{O1
PCI-37A M{nxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfROZYxNTZizszN NXz5XY4yPzJiaB?= MmXESG1UVw>? MnPMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NGLyZ44zOjNyN{ezOS=>
PCI-37B MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH1NYcxNTZizszN MWG3NkBp NHL5UVhFVVOR NHryPZdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHTXTGMzOjNyN{ezOS=>
PCI-15B NFzxVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzuVFkxNTZizszN NGLmeG04OiCq NGixRWhFVVOR NIDzdllqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NGDyRpgzOjNyN{ezOS=>
SCC-25 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[xU2lOOC14IN88US=> NU\XWHpvPzJiaB?= MX3EUXNQ MlnCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MVKyNlMxPzd|NR?=
UM-22A MVfGeY5kfGmxbjDBd5NigQ>? MYKwMVExKM7:TR?= MWGyOEBp NEHxb2FFVVOR NYDPOohscW6qaXLpeJMhfGinIHHjeIl3[XSrb36gc4YhfGinIFXHSnIhfHm{b4PpcoUhc2mwYYPlJIFv\CCjbIPvJIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDmc5JueyCxZjD0bIUh\G:5boP0doVidSC|aXfuZYxqdmdiZXzlcYVvfHNuIGPURXQ{KGGwZDDNRXBM NHXYXGozOjNyN{ezOS=>
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ACC3 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInjd5QxNTFyIN88US=> M{[1OlczKGh? MmC0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MV:xPFY6QDB{NR?=
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C666-1 M3PzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjXNE4yNTJ3Lk[g{txO MlzvOFghcA>? MoX0TWM2OD1{Mz60JO69VQ>? MXOxO|Y{OTZ2Nh?=
CNE-1 NXqyVYs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4niVlAvOS1{NT62JO69VQ>? M3fVdFczKGh? NEjkcVhKSzVyPUKuN{DPxE1? MnWzNVc3OzF4NE[=
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C666-1 M3nuOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHwS4dnOC5zLUK1MlYh|ryP MVW3NkBp NUKwN4hUUUN3ME20Mlg3KM7:TR?= Mk\DNVc3OzF4NE[=
CNE-1 NHu1RY1HfW6ldHnvckBCe3OjeR?= MlPmOkDPxE1? NV7qXmhWOjRiaB?= MXHk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= MUexO|Y{OTZ2Nh?=
CNE-2 M{i0XmZ2dmO2aX;uJGF{e2G7 M1\HVlYh|ryP NYf3dVNUOjRiaB?= MWHk[YxigXNiR{CvS|Eh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= NHP6[nUyPzZ|MU[0Oi=>
C666-1 MUDGeY5kfGmxbjDBd5NigQ>? MY[2JO69VQ>? MWCyOEBp NUnh[oJ[\GWuYYnzJGcxN0dzIHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NHXZfIIyPzZ|MU[0Oi=>

... Click to View More Cell Line Experimental Data

体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

+ 展开

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:

[1]

+ 展开
  • Cell lines: Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) 和 Lewis肺癌细胞
  • Concentrations: 0.1–100 μM
  • Incubation Time: 72 小时
  • Method:

    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。


    (Only for Reference)
动物实验:

[5]

+ 展开
  • 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
  • Formulation: 1% (v/v) 聚乙二醇溶液
  • Dosages: 12.5 mg/kg/day, 25 mg/kg/day, 50 mg/kg/day, 或 100 mg/kg/day
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 4 mg/mL (8.41 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% CMC Na
30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 475.35
化学式

C22H24BrFN4O2

CAS号 443913-73-3
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02495103 Recruiting Renal Cell Carcinoma|Hereditary Leiomyomatosis and Renal Cell Cancer|Papillary Renal Cell Carcinoma Sporadic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 8 2015 Phase 1|Phase 2
NCT00410761 Active not recruiting Thyroid Cancer Genzyme a Sanofi Company|Sanofi November 30 2006 Phase 3
NCT00537095 Active not recruiting Thyroid Neoplasms Genzyme a Sanofi Company|Sanofi September 29 2007 Phase 2
NCT00272350 Completed Recurrent High-Grade Gliomas|Progressive Low-Grade Gliomas|Malignant Gliomas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 29 2005 Phase 1
NCT01298323 Active not recruiting Locally Advanced or Metastatic Medullary Thyroid Cancer|Medullary Thyroid Cancer Genzyme a Sanofi Company|Sanofi February 25 2011 Phase 3
NCT02530411 Recruiting Neoplasms Velindre NHS Trust|Cancer Research UK|AstraZeneca April 2015 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID