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45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 NHTYT5dHfW6ldHnvckBCe3OjeR?= M4HsUlUxKM7:Zz;tcC=> MUSzNE83OC9zMkCgcYlv MV;pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gSmFMNCCVcnOgZY5lKEGtdB?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
HMEC-1  NF2yOJhHfW6ldHnvckBCe3OjeR?= M1qyb|IxNzRyL{[wJO69\y:vbB?= M1G4b4lvcGmkaYTzJGZCUyCjbnSgV5JkyqB? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
G44 MUDBdI9xfG:|aYOgRZN{[Xl? MVyxM|UwPTBizsznM41t NV;OTWVwOjRiaB?= M{TqO4lv\HWlZYOgZZBweHSxc3nz M2TkSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G28 MX\BdI9xfG:|aYOgRZN{[Xl? M3SxVVEwPS93MDFOwIcwdWx? MWmyOEBp NHTKTnZqdmS3Y3XzJIFxd3C2b4Ppdy=> M1PQTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G44 MkXrVJJwdGmoZYLheIlwdiCDc4PhfS=> MYexM|UwPTBizsznM41t MoTqNlQwPDhxN{KgbC=> M1HQT4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NFP0WZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G28 NEPI[JNRem:uaX\ldoF1cW:wIFHzd4F6 Mn6yNU82NzVyIN88[{9udA>? NYnG[FJSOjRxNEivO|IhcA>? MX7pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2W5[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1  NHT1VFJCeG:ydH;zbZMhSXO|YYm= MoD6NU82NzVyIN88[{9udA>? Mny1NlQhcA>? NH\NfWJqdmS3Y3XzJIFxd3C2b4Ppdy=> M3HGfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1  NIHZd4xRem:uaX\ldoF1cW:wIFHzd4F6 NFe0emwyNzVxNUCg{txoN22u NELLXJMzPC92OD:3NkBp NX;wbIRPcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MofhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
HMEC-1  MUjGeY5kfGmxbjDBd5NigQ>? NES3SFgyNzVxNUCg{txoN22u MV2yOEBp MV\pcoR2[2W|IHGg[I9{\SCmZYDlcoRmdnRiZHX0ZYNpdWWwdNMg NHi1cYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
LNT-229  NUfDU4RQTnWwY4Tpc44hSXO|YYm= M2iycFAvOS9zL{GwJO69VQ>? M2TSNVI1KGh? NE\KWYpqdXCjaYLzJJRp\SCjZHjld4lwdiCxZjDj[YxteyC2bzD2bZRzd26nY4TpckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NH\zflI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
T98G NVfrW|dVTnWwY4Tpc44hSXO|YYm= MVywMlEwOS9zMDFOwG0> M3m4O|I1KGh? MnvvbY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NFq3U3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
LN-18 NGTPdpdHfW6ldHnvckBCe3OjeR?= MnnxNE4yNzFxMUCg{txO M{XB[lI1KGh? MWXpcZBicXK|IITo[UBi\Ginc3nvckBw\iClZXzsd{B1dyC4aYTyc45m[3SrbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NYDSdpM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyNlEyPzFpPkG5NlIyOTdzPD;hQi=>
LN-308 NV72W4xMTnWwY4Tpc44hSXO|YYm= MlrTNE4yNzFxMUCg{txO MlvoNlQhcA>? MoPubY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NGW5XFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
U87MG MXvGeY5kfGmxbjDBd5NigQ>? M3TV[|AvOS9zL{GwJO69VQ>? NYPqcIFqOjRiaB?= M{HQRYlueGGrcoOgeIhmKGGmaHXzbY9vKG:oIHPlcIx{KHSxII\peJJwdmWldHnuJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MnPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO|EoRjF7MkKxNVcyRC:jPh?=
U87  NEO5fXhHfW6ldHnvckBCe3OjeR?= MoTsNE0zPSEQvHevcWw> MYSxNkBpyqB? M3m4[4lv\HWlZYOgZZV1d3CqYXf5JIRwe2ViZHXw[Y5l\W62bIm= M3j3T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251 M2nQXWZ2dmO2aX;uJGF{e2G7 M4DIbVAuOjVizsznM41N NXy2[lZuOTJiaNMg NWj3RY5VcW6mdXPld{BifXSxcHjh[5kh\G:|ZTDk[ZBmdmSnboTsfS=> MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U87  MWrBdI9xfG:|aYOgRZN{[Xl? NFjFdZczPSEQvHevcWw> M1KxWlI1NzR6IHi= MljZbY5lfWOnczDhdI9xfG:|aYOgZZQhPDhiaDDzbYdvcW[rY3HueIx6 MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd6OEO0N{c,OjF5OEizOFM9N2F-
U251 M{nKfmFxd3C2b4Ppd{BCe3OjeR?= MX:yOUDPxGdxbVy= NH3LV5ozPC92ODDo NF;OT2NqdmS3Y3XzJIFxd3C2b4Ppd{BifCB2ODDoJJNq\26rZnnjZY51dHl? M2jFbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U87  NVS5SYZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfNclNoOC1{NTFOwIcwdUx? M4DJc|AuPDhiaB?= MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK= M2jVXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2wMVI2KM7:Zz;tUC=> M3HBO|AuPDhiaB?= NVXyTHhzcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz M4P6XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251MG M2nxfmFxd3C2b4Ppd{BCe3OjeR?= MnS1NUDDvU1? M1vWUVQ5KGh? M{jhZolv\HWlZYOgZZBweHSxc3nz MnL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NUS4NFcoRjJ|M{W0PFA4RC:jPh?=
U87MG M3zzOWFxd3C2b4Ppd{BCe3OjeR?= M3HGdVEhyrWP NXLDdJNGPDhiaB?= M3TjS4lv\HWlZYOgZZBweHSxc3nz NXTZTZZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVQ5ODdpPkKzN|U1QDB5PD;hQi=>
U251MG M2PTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILmfGkxNTJ3IN88US=> MV6yOE81QCCq MX3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK= MnTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NUS4NFcoRjJ|M{W0PFA4RC:jPh?=
U87MG NWHaR|dzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[wMVI2KM7:TR?= NFeyWVgzPC92ODDo NWjl[mVxcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz MoXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NUS4NFcoRjJ|M{W0PFA4RC:jPh?=
MCF-7  NXfFT4d5SXCxcITvd4l{KEG|c3H5 NILwTHUxNTJyIN88US=> NICwZYs1QCCq Mk\zbY5lfWOnczDhdI9xfG:|aYO= NFeydWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1N|ExOid-MkSxOVMyODJ:L3G+
T-47D M1rZPWFxd3C2b4Ppd{BCe3OjeR?= NUXNToxTOC1{MDFOwG0> NFjoN2k1QCCq MYXpcoR2[2W|IHHwc5B1d3Orcx?= MmSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOxNFIoRjJ2MUWzNVAzRC:jPh?=
MCF-7  NG\XTphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XBSFAuOjBizszN MV[5OkBp MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFvq[2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1N|ExOid-MkSxOVMyODJ:L3G+
T-47D NIfZeXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXyNE0zOCEQvF2= NGGyNJY6PiCq NFPaN2NqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3M{GwNkc,OjRzNUOxNFI9N2F-
FaDu  NVq0dFJISXCxcITvd4l{KEG|c3H5 NF74T|YzPcLiwsXNxsA> NEO3Now1QMLiaNMg MoTFbY5lfWOnczDhdI9xfG:|aYO= NH7pS2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW1O|A2Pid-MkS1OVcxPTZ:L3G+
CAL27 M1yzVWFxd3C2b4Ppd{BCe3OjeR?= NGS2e2YzPcLiwsXNxsA> NIG5S281QMLiaNMg NHjBc29qdmS3Y3XzJIFxd3C2b4Ppdy=> MoXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
SCC25 M{PSXmFxd3C2b4Ppd{BCe3OjeR?= M3LmSVI2yqEEtV5CpC=> M2\iblQ5yqCqwrC= M3q5[4lv\HWlZYOgZZBweHSxc3nz MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
FaDu  NYDvVJRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnPOk4zPeLCk{KwNOKhyrWP MXG3NkBp MVHy[ZN2dHS|IH3v[IVz[XSnLDDkc5NmNWSncHXu[IVvfCCpcn;3eIghcW6qaXLpeIlwdg>? MmnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
CAL27 NV\MTHNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n3dVYvOjYkgKOyNFDDqML3TR?= MlvOO|IhcA>? NHK1OYFz\XO3bITzJI1w\GW{YYTlMEBld3OnLXTldIVv\GWwdDDndo94fGhiaX7obYJqfGmxbh?= NVL0R41xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
SCC25 NUnxV|ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn0Sow3NjJ34pETNlAxyqEEtV2= Mn7OO|IhcA>? NFjvPXJz\XO3bITzJI1w\GW{YYTlMEBld3OnLXTldIVv\GWwdDDndo94fGhiaX7obYJqfGmxbh?= MnjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
H28 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1LsNFEhdk1vMkCwJO69VQ>? NYfRbGJJPzJiaB?= MXjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1;o[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm1Nlc1Lz5{NEW5OVI4PDxxYU6=
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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