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 M3u4Z2Z2dmO2aX;uJGF{e2G7 NX;BNYF2PTBizsznM41t M4DxT|MxNzZyL{GyNEBucW5? NWLGepVHcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKE[DSzygV5JkKGGwZDDBb5Q> NWm2T5NrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
HMEC-1  M1jz[mZ2dmO2aX;uJGF{e2G7 NHfVcIQzOC92MD:2NEDPxGdxbXy= NXTvWIk1cW6qaXLpeJMhTkGNIHHu[EBUemQEoB?= NGW0N2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G44 MkHBRZBweHSxc3nzJGF{e2G7 MmruNU82NzVyIN88[{9udA>? NH[4RlIzPCCq NV2y[o1CcW6mdXPld{BieG:ydH;zbZM> M1faVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G28 M1zyOGFxd3C2b4Ppd{BCe3OjeR?= NGDyU4syNzVxNUCg{txoN22u MmToNlQhcA>? MWjpcoR2[2W|IHHwc5B1d3Orcx?= NIfGOm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G44 NYDrVVhGWHKxbHnm[ZJifGmxbjDBd5NigQ>? M3WzZlEwPS93MDFOwIcwdWx? M3T3TVI1NzR6L{eyJIg> MoO2bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1r3ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G28 MmjuVJJwdGmoZYLheIlwdiCDc4PhfS=> MmD4NU82NzVyIN88[{9udA>? NUm1VHh3OjRxNEivO|IhcA>? NFTMNIlqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MlXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
HMEC-1  M17Md2Fxd3C2b4Ppd{BCe3OjeR?= MW[xM|UwPTBizsznM41t M4W3NFI1KGh? MkP3bY5lfWOnczDhdI9xfG:|aYO= NIrxO3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1  M3KwN3Bzd2yrZnXyZZRqd25iQYPzZZk> MmTtNU82NzVyIN88[{9udA>? M3HkVVI1NzR6L{eyJIg> NYfyeJFScW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mk\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
HMEC-1  MmPHSpVv[3Srb36gRZN{[Xl? MWOxM|UwPTBizsznM41t NHnUXIIzPCCq NGLreWRqdmS3Y3XzJIEh\G:|ZTDk[ZBmdmSnboSg[IV1[WOqbXXueOKh NFPJfJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
LNT-229  M{CxcWZ2dmO2aX;uJGF{e2G7 MUiwMlEwOS9zMDFOwG0> MlfQNlQhcA>? NF3yR3lqdXCjaYLzJJRp\SCjZHjld4lwdiCxZjDj[YxteyC2bzD2bZRzd26nY4TpckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3nWfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkKxNVcyLz5zOUKyNVE4OTxxYU6=
T98G M4\6WmZ2dmO2aX;uJGF{e2G7 MnLzNE4yNzFxMUCg{txO MWeyOEBp M{fFdolueGGrcoOgeIhmKGGmaHXzbY9vKG:oIHPlcIx{KHSxII\peJJwdmWldHnuJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NVfNbop{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyNlEyPzFpPkG5NlIyOTdzPD;hQi=>
LN-18 Mn\CSpVv[3Srb36gRZN{[Xl? NGHsUFkxNjFxMT:xNEDPxE1? M1jD[lI1KGh? MkTHbY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MkmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO|EoRjF7MkKxNVcyRC:jPh?=
LN-308 MUPGeY5kfGmxbjDBd5NigQ>? NFXzdGcxNjFxMT:xNEDPxE1? MUCyOEBp M4\wTolueGGrcoOgeIhmKGGmaHXzbY9vKG:oIHPlcIx{KHSxII\peJJwdmWldHnuJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
U87MG NXviemMyTnWwY4Tpc44hSXO|YYm= M2TTWVAvOS9zL{GwJO69VQ>? NULUe5dqOjRiaB?= MoribY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
U87  MkfVSpVv[3Srb36gRZN{[Xl? M4HHU|AuOjVizsznM41N MmLINVIhcMLi NFnl[nJqdmS3Y3XzJIF2fG:yaHHnfUBld3OnIHTldIVv\GWwdHz5 Mlu5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251 M36wT2Z2dmO2aX;uJGF{e2G7 MlWwNE0zPSEQvHevcWw> M2PF[FEzKGkEoB?= NI\4ZpBqdmS3Y3XzJIF2fG:yaHHnfUBld3OnIHTldIVv\GWwdHz5 M2fvelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U87  Mk\tRZBweHSxc3nzJGF{e2G7 MmLyNlUh|rypL33M MkOyNlQwPDhiaB?= MUHpcoR2[2W|IHHwc5B1d3OrczDheEA1QCCqIIPp[45q\mmlYX70cJk> NU\idlNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PFg{PDNpPkKxO|g5OzR|PD;hQi=>
U251 NUT1WlB[SXCxcITvd4l{KEG|c3H5 M37wbVI2KM7:Zz;tUC=> MW[yOE81QCCq NHHKRnJqdmS3Y3XzJIFxd3C2b4Ppd{BifCB2ODDoJJNq\26rZnnjZY51dHl? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd6OEO0N{c,OjF5OEizOFM9N2F-
U87  MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrZNnMxNTJ3IN88[{9uVA>? M{DNNlAuPDhiaB?= M3PxOIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> Mk\BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251 M4POUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjNc2FVOC1{NTFOwIcwdUx? NHPQOm0xNTR6IHi= MlS5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy MnvqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251MG NVHjbVN{SXCxcITvd4l{KEG|c3H5 M1fndFEhyrWP MVK0PEBp NYS5S2U2cW6mdXPld{BieG:ydH;zbZM> NFPQWWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OFgxPyd-MkOzOVQ5ODd:L3G+
U87MG MYLBdI9xfG:|aYOgRZN{[Xl? M2fVVlEhyrWP NYjHTHdxPDhiaB?= NVfWRZZGcW6mdXPld{BieG:ydH;zbZM> NYHqSIJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVQ5ODdpPkKzN|U1QDB5PD;hQi=>
U251MG MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2S1ZVAuOjVizszN Mlf0NlQwPDhiaB?= NFrvVFVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN3NEiwO{c,OjN|NUS4NFc9N2F-
U87MG MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlSzNE0zPSEQvF2= MofyNlQwPDhiaB?= NHS0UllqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MnHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NUS4NFcoRjJ|M{W0PFA4RC:jPh?=
MCF-7  NYfiV5l2SXCxcITvd4l{KEG|c3H5 M174TVAuOjBizszN MnHNOFghcA>? MV7pcoR2[2W|IHHwc5B1d3Orcx?= NHu0VJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1N|ExOid-MkSxOVMyODJ:L3G+
T-47D MnviRZBweHSxc3nzJGF{e2G7 NGjyTW8xNTJyIN88US=> Moq3OFghcA>? NFnnO4lqdmS3Y3XzJIFxd3C2b4Ppdy=> M{DLWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUWzNVAzLz5{NEG1N|ExOjxxYU6=
MCF-7  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzQNFMxNTJyIN88US=> M1fLclk3KGh? NXGxdGNLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3M{GwNkc,OjRzNUOxNFI9N2F-
T-47D NUXyVpNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzpSZAxNTJyIN88US=> NWf2bWpyQTZiaB?= NGHDdJNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXW4dVl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMyODJpPkK0NVU{OTB{PD;hQi=>
FaDu  M37F[GFxd3C2b4Ppd{BCe3OjeR?= MUiyOeKhyrWPwrC= Mlf5OFjDqGkEoB?= NWTrTlZ[cW6mdXPld{BieG:ydH;zbZM> NFnR[Ik9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW1O|A2Pid-MkS1OVcxPTZ:L3G+
CAL27 NGDNSlNCeG:ydH;zbZMhSXO|YYm= MnTBNlXDqML3TdMg NWHNeW0zPDkEoHlCpC=> MVjpcoR2[2W|IHHwc5B1d3Orcx?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
SCC25 M3:1RmFxd3C2b4Ppd{BCe3OjeR?= MXWyOeKhyrWPwrC= MmTGOFjDqGkEoB?= NF;nVIxqdmS3Y3XzJIFxd3C2b4Ppdy=> NH3aPHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW1O|A2Pid-MkS1OVcxPTZ:L3G+
FaDu  Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX22MlI26oDVMkCwxsDDvU1? MWK3NkBp MkfUdoV{fWy2czDtc4RmemG2ZTyg[I9{\S2mZYDlcoRmdnRiZ4Lve5RpKGmwaHnibZRqd25? MoewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
CAL27 NI\DS3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3sUFY3NjJ34pETNlAxyqEEtV2= MmGyO|IhcA>? NG\LPItz\XO3bITzJI1w\GW{YYTlMEBld3OnLXTldIVv\GWwdDDndo94fGhiaX7obYJqfGmxbh?= NXWxVnJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
SCC25 NGTDcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYS2MlI26oDVMkCwxsDDvU1? M1\UbVczKGh? NXj0ZYdPemW|dXz0d{Bud2SncnH0[Uwh\G:|ZT3k[ZBmdmSnboSg[5Jwf3SqIHnubIljcXSrb36= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
H28 NXXme2hLS2WubDDWbYFjcWyrdImgRZN{[Xl? M3\oPFEhdk1vMkCwJO69VQ>? MmnIO|IhcA>? NGL3RXhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NUjEe|J1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVUzPzRpPkK0OVk2Ojd2PD;hQi=>
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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、SDS / 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、SDS / 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