Cilengitide trifluoroacetate

Catalog No.S7077 Synonyms: EMD 121974, NSC 707544

For research use only.

Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

Cilengitide trifluoroacetate Chemical Structure

CAS No. 199807-35-7

Selleck's Cilengitide trifluoroacetate has been cited by 52 publications

Purity & Quality Control

Choose Selective Integrin Inhibitors

Biological Activity

Description Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.
Targets
αvβ3 receptor [1]
(Cell-free assay)
αvβ5 receptor [2]
(Cell-free assay)
4.1 nM 79 nM
In vitro

Cilengitide is a cyclized pentapeptide peptidomimetic designed to compete for the arginine-glycine-aspartic acid (RGD) peptide sequence that regulates integrin-ligand binding. Cilengitide selectively and potently blocks the ligation of theαvβ3 andαvβ5 integrins to provisional matrix proteins such as vitronectin, fibronectin, fibrinogen, von Willebrand factor, osteopontin, and others. [1] Cilegitide inhibits angiogenesis in vitro. 10 μM Cilengitide completely inhibits attachment of BAE, BME and HUVE cells on vitronectin and fibronectin. Cilengitide inhibits in vitro angiogenesis of BAE cells on three-dimensional collagen and fibrin gels pretreated with FGF-2(or VEGF-A) with IC50 of 15 μM and 8 μM, 4 μM and 3 μM, respectively. [2] Cilengitide blocks proliferation and induces apoptosis of endothelial cells as well as differentiation of human endothelial precursor cells (EPCs). 50 μg/mL Cilengitide completely inhibits the proliferation of human microvascular endothelial cell line HMEC-1 and leads to apoptosis in ~30% cells. [3] 1.0 μM Cilengitide treating for 9 days inhibits the proliferation of EPCs by nearly 40%. 1 μM Cilengitide inhibits the differentiation of EPCs by more than 80% at 14 days. [4] Cilengitide inhibits adhesion and induces apoptosis of tumor cells. 25 μg/mL Cilengitide causes detachment of DAOY cells (medulloblastoma) and U87MG cells (glioblastoma) from vitronectin and tenascin by more than 60%. 25 μg/mL Cilengitide induces a nearly 50% apoptosis rate of these cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
G28 MVPGeY5kfGmxbjDBd5NigQ>? Mk\sOVAh|rypL33s NHPBS|M{OC94MD:xNlAhdWmw MlHObY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGZCUyxiU4LjJIFv\CCDa4S= MnP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMUSwNFUoRjF7MUG0NFA2RC:jPh?=
HMEC-1  MonISpVv[3Srb36gRZN{[Xl? MoHtNlAwPDBxNkCg{txoN22u Mn3XbY5pcWKrdIOgSmFMKGGwZDDTdoPDqA>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
G44 MUjBdI9xfG:|aYOgRZN{[Xl? MmLlNU82NzVyIN88[{9udA>? NUG1PJhiOjRiaB?= MoPlbY5lfWOnczDhdI9xfG:|aYO= M3zMOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G28 M3;JVGFxd3C2b4Ppd{BCe3OjeR?= M{LYWFEwPS93MDFOwIcwdWx? MXKyOEBp MX;pcoR2[2W|IHHwc5B1d3Orcx?= M2Tp[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
G44 NWrkfplkWHKxbHnm[ZJifGmxbjDBd5NigQ>? NXG0eI5JOS93L{WwJO69\y:vbB?= MmXrNlQwPDhxN{KgbC=> MlrpbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFvlTmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G28 MWHQdo9tcW[ncnH0bY9vKEG|c3H5 MnXNNU82NzVyIN88[{9udA>? NVXUPWVGOjRxNEivO|IhcA>? NGPHSJNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NHvQOZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1  NEnI[nVCeG:ydH;zbZMhSXO|YYm= NH7mVJgyNzVxNUCg{txoN22u Mn\JNlQhcA>? NFLWfmtqdmS3Y3XzJIFxd3C2b4Ppdy=> NGrOfII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1  NF74V3RRem:uaX\ldoF1cW:wIFHzd4F6 Moe1NU82NzVyIN88[{9udA>? NFzxNoozPC92OD:3NkBp MnjzbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2P3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1  NFGweW1HfW6ldHnvckBCe3OjeR?= MmrRNU82NzVyIN88[{9udA>? Mk[1NlQhcA>? NGK2[VVqdmS3Y3XzJIEh\G:|ZTDk[ZBmdmSnboSg[IV1[WOqbXXueOKh NVrPOHM1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
LNT-229  NW\OTFlNTnWwY4Tpc44hSXO|YYm= MlHvNE4yNzFxMUCg{txO NGTJb4gzPCCq NGrRVHVqdXCjaYLzJJRp\SCjZHjld4lwdiCxZjDj[YxteyC2bzD2bZRzd26nY4TpckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
T98G NEfKVWRHfW6ldHnvckBCe3OjeR?= NVvMepBjOC5zL{GvNVAh|ryP MlLGNlQhcA>? NEHPc5BqdXCjaYLzJJRp\SCjZHjld4lwdiCxZjDj[YxteyC2bzD2bZRzd26nY4TpckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3vITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkKxNVcyLz5zOUKyNVE4OTxxYU6=
LN-18 M3LIUWZ2dmO2aX;uJGF{e2G7 MkPhNE4yNzFxMUCg{txO M4fJe|I1KGh? MnnJbY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Ml7rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO|EoRjF7MkKxNVcyRC:jPh?=
LN-308 Mn7nSpVv[3Srb36gRZN{[Xl? M13BUlAvOS9zL{GwJO69VQ>? NUDnb2JKOjRiaB?= MXPpcZBicXK|IITo[UBi\Ginc3nvckBw\iClZXzsd{B1dyC4aYTyc45m[3SrbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ{MUG3NUc,OTl{MkGxO|E9N2F-
U87MG MnrDSpVv[3Srb36gRZN{[Xl? MkDrNE4yNzFxMUCg{txO MoLWNlQhcA>? NWnzfJk6cW2yYXnyd{B1cGViYXTo[ZNqd25ib3[gZ4VtdHNidH:geol1em:wZXP0bY4hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Moj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO|EoRjF7MkKxNVcyRC:jPh?=
U87  Mm\3SpVv[3Srb36gRZN{[Xl? NVrBd|BYOC1{NTFOwIcwdUx? MoDwNVIhcMLi MmXCbY5lfWOnczDheZRweGijZ4mg[I9{\SCmZYDlcoRmdnSueR?= M4nETVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251 MkDVSpVv[3Srb36gRZN{[Xl? NXHmXGxZOC1{NTFOwIcwdUx? NFXp[28yOiCqwrC= MWnpcoR2[2W|IHH1eI9xcGGpeTDkc5NmKGSncHXu[IVvfGy7 M1rpOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U87  M3nx[2Fxd3C2b4Ppd{BCe3OjeR?= NXr1bnBEOjVizsznM41N NHXySmYzPC92ODDo NXnYVI5{cW6mdXPld{BieG:ydH;zbZMh[XRiNEigbEB{cWewaX\pZ4FvfGy7 NF3uXZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe4PFM1Oyd-MkG3PFg{PDN:L3G+
U251 Ml3rRZBweHSxc3nzJGF{e2G7 NXP0[oxmOjVizsznM41N M3PXblI1NzR6IHi= NYXGNoZWcW6mdXPld{BieG:ydH;zbZMh[XRiNEigbEB{cWewaX\pZ4FvfGy7 NVmwTFU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PFg{PDNpPkKxO|g5OzR|PD;hQi=>
U87  NV;i[YpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL4NE0zPSEQvHevcWw> Mmj3NE01QCCq NYniW2xzcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz MlHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N|Q{RC:jPh?=
U251 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnJfmM5OC1{NTFOwIcwdUx? MWOwMVQ5KGh? MnfEbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy M{jiXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N|Q{Lz5{MUe4PFM1OzxxYU6=
U251MG MoLaRZBweHSxc3nzJGF{e2G7 MmCwNUDDvU1? M{\sPFQ5KGh? NEfL[|VqdmS3Y3XzJIFxd3C2b4Ppdy=> NUDPS2RoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVQ5ODdpPkKzN|U1QDB5PD;hQi=>
U87MG M2G0WGFxd3C2b4Ppd{BCe3OjeR?= Mk\xNUDDvU1? NFX5bIE1QCCq M3jSeIlv\HWlZYOgZZBweHSxc3nz MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN3NEiwO{c,OjN|NUS4NFc9N2F-
U251MG NInqfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\BRXBmOC1{NTFOwG0> NUPmeYlKOjRxNEigbC=> NXznVnlPcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN3NEiwO{c,OjN|NUS4NFc9N2F-
U87MG NIHxSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7tcGcxNTJ3IN88US=> MnnKNlQwPDhiaB?= NWGzUZNJcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz NWr3XHlnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVQ5ODdpPkKzN|U1QDB5PD;hQi=>
MCF-7  MXLBdI9xfG:|aYOgRZN{[Xl? NUfXcGhvOC1{MDFOwG0> MXi0PEBp NVrmZmZFcW6mdXPld{BieG:ydH;zbZM> MnTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOxNFIoRjJ2MUWzNVAzRC:jPh?=
T-47D M1zGemFxd3C2b4Ppd{BCe3OjeR?= MUSwMVIxKM7:TR?= M4XjW|Q5KGh? M1LzSolv\HWlZYOgZZBweHSxc3nz M{Lh[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUWzNVAzLz5{NEG1N|ExOjxxYU6=
MCF-7  Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMVIxKM7:TR?= MoTaPVYhcA>? MnHubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M3jKNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUWzNVAzLz5{NEG1N|ExOjxxYU6=
T-47D Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIKwcXkxNTJyIN88US=> NEK0fXE6PiCq MULpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NUGweY92RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMyODJpPkK0NVU{OTB{PD;hQi=>
FaDu  NEC2S3hCeG:ydH;zbZMhSXO|YYm= M37NcFI2yqEEtV5CpC=> NFm5Wmo1QMLiaNMg M1XsWolv\HWlZYOgZZBweHSxc3nz NUH0XWxbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
CAL27 M1n5emFxd3C2b4Ppd{BCe3OjeR?= NFjLdGgzPcLiwsXNxsA> NH3O[mg1QMLiaNMg MVXpcoR2[2W|IHHwc5B1d3Orcx?= MmLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
SCC25 M37SS2Fxd3C2b4Ppd{BCe3OjeR?= MY[yOeKhyrWPwrC= NHThbWc1QMLiaNMg M122T4lv\HWlZYOgZZBweHSxc3nz MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
FaDu  M{Ttdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWOz[Y11Pi5{NfMAl|IxOMLiwsXN MmfTO|IhcA>? MULy[ZN2dHS|IH3v[IVz[XSnLDDkc5NmNWSncHXu[IVvfCCpcn;3eIghcW6qaXLpeIlwdg>? MnLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NUewOVYoRjJ2NUW3NFU3RC:jPh?=
CAL27 MnTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfCbIQ3NjJ34pETNlAxyqEEtV2= MmnJO|IhcA>? Mnf4doV{fWy2czDtc4RmemG2ZTyg[I9{\S2mZYDlcoRmdnRiZ4Lve5RpKGmwaHnibZRqd25? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV3N{C1Okc,OjR3NUewOVY9N2F-
SCC25 NUnOe2xNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYe2MlI26oDVMkCwxsDDvU1? M4W1TFczKGh? NWnVWllSemW|dXz0d{Bud2SncnH0[Uwh\G:|ZT3k[ZBmdmSnboSg[5Jwf3SqIHnubIljcXSrb36= NVfk[Hc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
H28 NVzRZ496S2WubDDWbYFjcWyrdImgRZN{[Xl? NEHQOmUyKG6PLUKwNEDPxE1? MoDVO|IhcA>? MXvk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NInjcXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVI4PCd-MkS1PVUzPzR:L3G+
MM05 Mkj5R4VtdCCYaXHibYxqfHliQYPzZZk> M1rlcVEhdk1vMkCwJO69VQ>? NVLSbJNWPzJiaB?= NWHzWVA4\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NH\S[FA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVI4PCd-MkS1PVUzPzR:L3G+
MSTO-211H MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWexJI5ONTJyMDFOwG0> M1P1e|czKGh? NIizWG5l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NFrne|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW5OVI4PCd-MkS1PVUzPzR:L3G+
REN MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NV\p[|I3OSCwTT2yNFAh|ryP MYS3NkBp NV\rTIJE\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NWfrc2JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PVUzPzRpPkK0OVk2Ojd2PD;hQi=>
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Assay
Methods Test Index PMID
Western blot pFAK / p-AKT ; GLI1 19114005 31366904
Immunofluorescence VE-cadherin / β3 integrin 19212436
Growth inhibition assay Cell number 24153102
In vivo Cilengitide is activity against tumor growth and angiogenesis as single-agent. 100 μg Cilengitide induces a significant decrease in the number of CD 31+ vessels seen in tumors (2/high-power field) compared with control tumors (56/high-power field). 100 μg Cilengitide increases cellular apoptosis in the brain tumors of animals (2.2% apoptotic cells/high-power field) compared with those receiving the inactive peptide (1.7% cells/high-power field). Cilengitide treatment results in prolonged survival of the mice bearing melanoma xenografts M21 compared with control treatment group. (36.5 vs 17.3 days). [5] Cilengitide can augment the therapeutic benefit associated with cytotoxic agents including chemotherapy and radiation therapy in tumor models. Cilengitide (250 mg/dose) alone does not alter tumor growth of breast cancer xenografts when compared with untreated mice, but combined modality RIT (CMRIT) using RIT and six doses of Cilengitide (250 mg/dose) increases efficacy of treatment, with the cure rate for mice that receives only RIT increasing from 15 to 53%. CMRIT significantly increases apoptosis of tumor and endothelial cells 5 days, and decreases tumor proliferation. [6]

Protocol (from reference)

Kinase Assay:[2]
  • Integrin-binding competition assay:

    Recombinant soluble integrins are immobilized, and peptides, which are serially diluted in Tris-buffered saline (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), are added in parallel with biotinylated vitronectin (to 1μg/mL). After a 3-h incubation at 37℃ and washing with Tris–buffered saline, bound ligand is detected by incubation with an antibiotin alkaline phosphatase-conjugated antibody (BioRad) followed by development with p-nitrophenyl phosphatase substrate. The reaction is stopped by the addition of NaOH and the color intensity read at 405 nm.

Cell Research:[3]
  • Cell lines: Human microvascular endothelial cell line HMEC-1
  • Concentrations: 1-50 μg/mL
  • Incubation Time: 3 days
  • Method: HMEC-1 (1×104 per well) are seeded on uncoated 48 well plates and incubated in medium containing 4% FCS with Cilengitide. After incubation for 72 hours at 37℃, cells are trypsinized and counted.
  • (Only for Reference)
Animal Research:[5]
  • Animal Models: Human glioblastoma xenografts U87 MG
  • Dosages: 100μg
  • Administration: Daily i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 702.68
Formula

C29H41F3N8O9

CAS No. 199807-35-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N.C(=O)(C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 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?

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

Question 2:
Is Cilengitide a TFA salt?

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

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