Cilengitide trifluoroacetate

For research use only. Not for use in humans.

目录号:S7077 别名: EMD 121974, NSC 707544 中文名称:三氟醋酸盐西仑吉肽

Cilengitide trifluoroacetate Chemical Structure

CAS No. 199807-35-7

Cilengitide (EMD 121974, NSC 707544)是一种有效的integrin抑制剂,作用于αvβ3受体和αvβ5受体,无细胞试验中IC50分别为4.1 nM和79 nM,比作用于gpIIbIIIa选择性高10倍左右。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3718.02 现货
RMB 2212.59 现货
RMB 8108.38 现货
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客户使用Selleck生产的Cilengitide trifluoroacetate发表文献46篇:

产品安全说明书

Integrin抑制剂选择性比较

生物活性

产品描述 Cilengitide (EMD 121974, NSC 707544)是一种有效的integrin抑制剂,作用于αvβ3受体和αvβ5受体,无细胞试验中IC50分别为4.1 nM和79 nM,比作用于gpIIbIIIa选择性高10倍左右。Phase 2。
靶点
αvβ3 receptor [1]
(Cell-free assay)
αvβ5 receptor [2]
(Cell-free assay)
4.1 nM 79 nM
体外研究

Cilengitide是一种环化五胜肽类肽,争夺精氨酸-甘氨酸-天冬氨酸(RGD)肽序列。调节整合素-配体结合。Cilengitide选择性且有效抑制αvβ3和αvβ5整合素与基质蛋白结合,如Vitronectin, Fibronectin, Fibrinogen, von Willebrand Factor, Osteopontin, 及其他。[1]10 μM Cilengitide完全抑制BAE,BME和HUVE细胞与Vitronectin 和 Fibronectin附着。Cilengitide在体外作用于三维胶原蛋白和血纤维蛋白凝胶使用FGF-2(或 VEGF-A)预处理的BAE细胞,抑制血管生成,IC50分别为15 μM 和8 μM, 4 μM 和 3 μM。[2]Cilengitide 抑制细胞增殖,诱导内皮细胞凋亡,且诱导人体内皮前体细胞分化。50 μg/mL Cilengitide完全抑制人体微血管内皮细胞系HMEC-1增殖,导致〜30%细胞发生细胞凋亡。[3]1 μM Cilengitide处理9天,抑制近40%EPCs增殖。1 μM Cilengitide处理14天,抑制80%以上EPCs 分化。[4]Cilengitide抑制粘附,诱导肿瘤细胞凋亡。25 μg/mL Cilengitide使60%以上的DAOY细胞(髓母细胞瘤)和U87MG细胞(胶质母细胞瘤) 与Vitronectin 和 Tenascin分离。25 μg/mL Cilengitide诱导细胞凋亡率将近50% 。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
G28 NGLieYNHfW6ldHnvckBCe3OjeR?= M{mxOFUxKM7:Zz;tcC=> NWfTb4ZYOzBxNkCvNVIxKG2rbh?= MUjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gSmFMNCCVcnOgZY5lKEGtdB?= NH3iWZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1  MUjGeY5kfGmxbjDBd5NigQ>? M2XqU|IxNzRyL{[wJO69\y:vbB?= MUXpcohq[mm2czDGRWsh[W6mIGPyZ:Kh NVfU[XA5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
G44 MVnBdI9xfG:|aYOgRZN{[Xl? NUCzdXRrOS93L{WwJO69\y:vbB?= NUS0cJJZOjRiaB?= NVjzbYhrcW6mdXPld{BieG:ydH;zbZM> MmTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
G28 M1m0TWFxd3C2b4Ppd{BCe3OjeR?= NVTSTolUOS93L{WwJO69\y:vbB?= MnriNlQhcA>? NFfZNIpqdmS3Y3XzJIFxd3C2b4Ppdy=> MmPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
G44 M4[3TXBzd2yrZnXyZZRqd25iQYPzZZk> NYX0XW5vOS93L{WwJO69\y:vbB?= M4HLTlI1NzR6L{eyJIg> NF\FUYtqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NGnkXZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G28 NXLvRY1FWHKxbHnm[ZJifGmxbjDBd5NigQ>? M121blEwPS93MDFOwIcwdWx? MWiyOE81QC95MjDo M37UWolvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3rNbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1  NH31NWRCeG:ydH;zbZMhSXO|YYm= MorJNU82NzVyIN88[{9udA>? M2XMWVI1KGh? NWfhNnh1cW6mdXPld{BieG:ydH;zbZM> M1qxR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1  MmHxVJJwdGmoZYLheIlwdiCDc4PhfS=> NEHVV4cyNzVxNUCg{txoN22u NEKxemIzPC92OD:3NkBp MlTBbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
HMEC-1  MXrGeY5kfGmxbjDBd5NigQ>? MUexM|UwPTBizsznM41t MlPPNlQhcA>? Ml7TbY5lfWOnczDhJIRwe2ViZHXw[Y5l\W62IHTleIFkcG2nboVCpC=> NXvPd4JPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
LNT-229  NHP5d3BHfW6ldHnvckBCe3OjeR?= NFLjZVYxNjFxMT:xNEDPxE1? Mnj1NlQhcA>? NVjVVWl2cW2yYXnyd{B1cGViYXTo[ZNqd25ib3[gZ4VtdHNidH:geol1em:wZXP0bY4hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
T98G M{PxemZ2dmO2aX;uJGF{e2G7 NFPScpkxNjFxMT:xNEDPxE1? NUHiXVNlOjRiaB?= NWroV2p1cW2yYXnyd{B1cGViYXTo[ZNqd25ib3[gZ4VtdHNidH:geol1em:wZXP0bY4hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NFiwboU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
LN-18 MlzLSpVv[3Srb36gRZN{[Xl? M1XX[VAvOS9zL{GwJO69VQ>? NWK4dnFbOjRiaB?= MXLpcZBicXK|IITo[UBi\Ginc3nvckBw\iClZXzsd{B1dyC4aYTyc45m[3SrbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NGq2W5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
LN-308 NVfMXJM1TnWwY4Tpc44hSXO|YYm= MX:wMlEwOS9zMDFOwG0> NWXnW21jOjRiaB?= Ml\kbY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
U87MG M1HsOWZ2dmO2aX;uJGF{e2G7 NWLifFB6OC5zL{GvNVAh|ryP MVmyOEBp M1i3UIlueGGrcoOgeIhmKGGmaHXzbY9vKG:oIHPlcIx{KHSxII\peJJwdmWldHnuJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NWS3WG9tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyNlEyPzFpPkG5NlIyOTdzPD;hQi=>
U87  NXS2eYJqTnWwY4Tpc44hSXO|YYm= NF3wN2oxNTJ3IN88[{9uVA>? NGG0VHQyOiCqwrC= M{TOcYlv\HWlZYOgZZV1d3CqYXf5JIRwe2ViZHXw[Y5l\W62bIm= M4DTVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251 M2PyRWZ2dmO2aX;uJGF{e2G7 MYSwMVI2KM7:Zz;tUC=> NUSzdlQ2OTJiaNMg NV\LboVvcW6mdXPld{BifXSxcHjh[5kh\G:|ZTDk[ZBmdmSnboTsfS=> M3jSWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U87  NEf5XJpCeG:ydH;zbZMhSXO|YYm= NUPrclZSOjVizsznM41N MV:yOE81QCCq MmDobY5lfWOnczDhdI9xfG:|aYOgZZQhPDhiaDDzbYdvcW[rY3HueIx6 MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd6OEO0N{c,OjF5OEizOFM9N2F-
U251 NYfJPGRCSXCxcITvd4l{KEG|c3H5 MkHlNlUh|rypL33M MkPFNlQwPDhiaB?= NXrNTIR5cW6mdXPld{BieG:ydH;zbZMh[XRiNEigbEB{cWewaX\pZ4FvfGy7 Mn\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U87  MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDsOI0xNTJ3IN88[{9uVA>? NYrmbIFmOC12ODDo NG\2bmtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MnLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PhR|AuOjVizsznM41N M{nV[lAuPDhiaB?= MULpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK= Mmf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251MG M1\VVmFxd3C2b4Ppd{BCe3OjeR?= MVmxJOK2VQ>? NH7Vdlg1QCCq MoHIbY5lfWOnczDhdI9xfG:|aYO= M{\JSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{W0PFA4Lz5{M{O1OFgxPzxxYU6=
U87MG NEnNfpBCeG:ydH;zbZMhSXO|YYm= NIP4PYcyKML3TR?= NEjIS481QCCq NHHoU4RqdmS3Y3XzJIFxd3C2b4Ppdy=> NEfFb4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OFgxPyd-MkOzOVQ5ODd:L3G+
U251MG M4GyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUewMVI2KM7:TR?= NWjo[YVGOjRxNEigbC=> M2X0XIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> NYnIcWExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVQ5ODdpPkKzN|U1QDB5PD;hQi=>
U87MG MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Ppc|AuOjVizszN MYSyOE81QCCq M2\rNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> M4HmZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{W0PFA4Lz5{M{O1OFgxPzxxYU6=
MCF-7  MYDBdI9xfG:|aYOgRZN{[Xl? M3vMRVAuOjBizszN MmHmOFghcA>? NWfr[lE4cW6mdXPld{BieG:ydH;zbZM> MmHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOxNFIoRjJ2MUWzNVAzRC:jPh?=
T-47D NFv0b4dCeG:ydH;zbZMhSXO|YYm= M3nIPVAuOjBizszN NG\O[201QCCq NH2xO5JqdmS3Y3XzJIFxd3C2b4Ppdy=> NFvm[VI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1N|ExOid-MkSxOVMyODJ:L3G+
MCF-7  NULFTVFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnINE0zOCEQvF2= M4TrNlk3KGh? NX32TWFWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOxNFIoRjJ2MUWzNVAzRC:jPh?=
T-47D M3\Bfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMVIxKM7:TR?= MVW5OkBp NHvQNItqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3M{GwNkc,OjRzNUOxNFI9N2F-
FaDu  MYDBdI9xfG:|aYOgRZN{[Xl? NE\penczPcLiwsXNxsA> MUW0POKhcMLi M2Hqe4lv\HWlZYOgZZBweHSxc3nz MojiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
CAL27 MUnBdI9xfG:|aYOgRZN{[Xl? MoLUNlXDqML3TdMg NU\xPYNDPDkEoHlCpC=> NG\MWnlqdmS3Y3XzJIFxd3C2b4Ppdy=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
SCC25 NVHFSZprSXCxcITvd4l{KEG|c3H5 NEfldYMzPcLiwsXNxsA> NXHzXnh{PDkEoHlCpC=> MWDpcoR2[2W|IHHwc5B1d3Orcx?= NWD3T5p7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
FaDu  NVS1d3NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe2MlI26oDVMkCwxsDDvU1? NEL1To04OiCq NIDMSoVz\XO3bITzJI1w\GW{YYTlMEBld3OnLXTldIVv\GWwdDDndo94fGhiaX7obYJqfGmxbh?= NVGzWZpKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
CAL27 M4iy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPLOk4zPeLCk{KwNOKhyrWP NIO4dIo4OiCq MVfy[ZN2dHS|IH3v[IVz[XSnLDDkc5NmNWSncHXu[IVvfCCpcn;3eIghcW6qaXLpeIlwdg>? M4TlVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUW3NFU3Lz5{NEW1O|A2PjxxYU6=
SCC25 NHvJbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PSb|YvOjYkgKOyNFDDqML3TR?= NHT6[3c4OiCq NELBUnlz\XO3bITzJI1w\GW{YYTlMEBld3OnLXTldIVv\GWwdDDndo94fGhiaX7obYJqfGmxbh?= M4XlOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUW3NFU3Lz5{NEW1O|A2PjxxYU6=
H28 NGrUZWNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoXDNUBvVS1{MECg{txO MVi3NkBp MUjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7NUK3OEc,OjR3OUWyO|Q9N2F-
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFAK / p-AKT ; 

PubMed: 19114005     


G28 cells were treated with 50 μg/ml cilengitide for 30, 60 and 120 minutes at 37°C. Cell lysates containing similar amounts of protein were separated by SDS-PAGE, transferred to a nitrocellulose membrane and probed with specific antibodies for detection of β-actin and phosphorylated FAK and Akt.

GLI1; 

PubMed: 31366904     


Western blottingting showing downregulated GLI1 with Integrin αvβ3 inhibitor Cilengitide and upregulated GLI1 with co-stimulator ligand RGD compared to the blank control in SGC7901 MCAs and BGC823 MCAs. 

19114005 31366904
Immunofluorescence
VE-cadherin / β3 integrin ; 

PubMed: 19212436     


Confluent HUVEC plated on fibronectin or collagen I were exposed to cilengitide (10 µM each) for the indicated time and double stained for VE-cadherin and β3 integrin. Cilengitide disrupted VE-cadherin staining and promoted appearance of β3 at VE-cadherin-depleted cell-cell borders. Higher magnification of HUVEC cultures demonstrate rare co-localization of VE-cadherin and β3 integrin at cellular junctions upon cilengitide stimulation (arrowheads). Bars: 10 µm.

19212436
Growth inhibition assay
Cell number ; 

PubMed: 24153102     


Cell detachment following 1 hr Cilengitide treatment. Cells were treated with cilengitide for 1 hr, washed with PBS, and remaining attached cells were trypsinized and counted. A) T-47D cells showed a strong dose response, with almost complete cell detachment at 20 uM cilengitide treatment. B) MCF-7 cells showed moderate cell detachment similar to C) MDA-MB-231 cells. D) MDA-MB-468 cells showed little to no cell detachment following this short exposure to cilengitide. Figures show Mean ± SEM and represent the average of three experiments. * = ≤ 0.05.

24153102
体内研究 Cilengitide单独处理,有效对抗肿瘤生长和血管生成。100 μg Cilengitide处理肿瘤,与对照组相比,显著降低CD31+血管数。100 μg Cilengitide处理动物大脑中的肿瘤,与接收无效肽处理的相比,促进细胞凋亡。Cilengitide 处理携带黑色素移植瘤M21的小鼠,对照组相比,延长小鼠寿命,分别为36.5 天vs 17.3天。[5]Cilengitide 可以增加细胞毒性药物相关联的治疗的益处,包括对肿瘤模型的化疗和放射治疗。Cilengitide (250 mg/dose)单独处理小鼠,与未经处理的小鼠相比,没有改变乳腺癌移植瘤的肿瘤生长,但与RIT(CMRIT)联合治疗,使用RIT和六种剂量的Cilengitide (250 mg/dose)增加治疗的疗效,小鼠的治愈率从只用RIT处理的 15%提高到53%。CMRIT处理内皮细胞5天,显著促进肿瘤细胞凋亡,且降低肿瘤细胞增殖。[6]

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:[2]
- 合并

整合素竞争结合实验:

固定化重组可溶性的整合素,同时加入在Tris 缓冲生理盐水(TBS++) (0.1% (w/v) BSA, 150 mM NaCl, 1 mM CaCl2, 1 mM MgCl2 10 μM MnCl2, 20 mM Tris-HCl; pH 7.4)中连续稀释的肽,及生物素化的Vitronectin(1μg/mL)。在37°C下温育3小时后,使用Tris 缓冲生理盐水洗涤,通过与抗生物素的碱性磷酸酶联合的抗体温育,再经对硝基苯基磷酸酶底物显影,测定结合的配体。加入NaOH终止反应,在405 nm处读取彩色信号强度。
细胞实验:[3]
- 合并
  • Cell lines: 人体微血管内皮细胞系HMEC-1
  • Concentrations: 1-50 μg/mL
  • Incubation Time: 3 天
  • Method: HMEC-1 按每孔1×104个接种在未包被的48孔板中,在含4% FCS 及 Cilengitide的培养基中温育。在37°C下温育72小时, 用胰蛋白酶处理细胞并计数。
    (Only for Reference)
动物实验:[5]
- 合并
  • Animal Models: 携带人体胶质母细胞瘤移植瘤U87 MG的小鼠
  • Dosages: 100μg
  • Administration: 每天腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (142.31 mM)
Water 8 mg/mL (11.38 mM)
Ethanol Insoluble

* 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 702.68
化学式

C29H41F3N8O9

CAS号 199807-35-7
储存条件 粉状
溶于溶剂
别名 EMD 121974, NSC 707544

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01517776 Terminated Drug: Cilengitide|Drug: Temozolomide Gliomas Martin-Luther-Universität Halle-Wittenberg|Merck KGaA Darmstadt Germany January 2012 Phase 2
NCT01118676 Completed Drug: cilengitide radiochemotherapy Locally Advanced Non Small Cell Lung Cancer (NSCLC)* Institut Claudius Regaud|Merck KGaA Darmstadt Germany March 2010 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    The recommend vehicle is 30% propylene glycol, 5% Tween 80, 65% D5W at 30mg/ml, can you let me know if this is a suspension or clear solution?

  • 回答:

    S7077 Cilengitide can be dissolved in 30% propylene glycol/5% Tween 80/65% D5W at 10 mg/ml as a clear solution.

  • 问题 2:

    Is Cilengitide a TFA salt?

  • 回答:

    S7077 Cilengitide is actually a TFA salt, and the ratio between Cilengitide and TFA is 1:1.

Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID