Cilengitide trifluoroacetate

Name: Cilengitide trifluoroacetate
Brand: Selleck Chemicals
SKU: S7077
Rating: 5 (46 reviews)

For research use only.

Catalog No.S7077 Synonyms: EMD 121974, NSC 707544

46 publications

Cilengitide trifluoroacetate Chemical Structure

CAS No. 199807-35-7

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.

Selleck's Cilengitide trifluoroacetate has been cited by 46 publications

Nat Genet, 2019, 51(9):1389-1398

PubMed: 31477929 ( click the link to review the publication )

Cell Prolif, 2021, 54(4):e13012

PubMed: 33656760 ( click the link to review the publication )

Acta Biochim Biophys Sin (Shanghai), 2021, 53(3):294-303

PubMed: 33493267 ( click the link to review the publication )

Exp Brain Res, 2021, 10.1007/s00221-021-06111-x

PubMed: 33991211 ( click the link to review the publication )

Clin Transl Med, 2021, 11(2):e295

PubMed: 33634976 ( click the link to review the publication )

Cell Death Discov, 2020, 6:86

PubMed: 33014430 ( click the link to review the publication )

J Cell Sci, 2020,

PubMed: 32788230 ( click the link to review the publication )

J Cell Mol Med, 2020, 24(2):1460-1473

PubMed: 31828970 ( click the link to review the publication )

J Cell Mol Med, 2020, 24(1):996-1009

PubMed: 31701659 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(18)E6913

PubMed: 32967150 ( click the link to review the publication )

J Biol Chem, 2020, 12 pii: jbc

PubMed: 32280065 ( click the link to review the publication )

Exp Dermatol, 2020, 16

PubMed: 32298492 ( click the link to review the publication )

Blood Adv, 2020, 4(6):1021-1037

PubMed: 32191808 ( click the link to review the publication )

Theranostics, 2019, 9(5):1264-1279

PubMed: 30867829 ( click the link to review the publication )

Nanoscale, 2019, 11(39):18224-18231

PubMed: 31560005 ( click the link to review the publication )

Cell Death Dis, 2019, 10(8):574

PubMed: 31366904 ( click the link to review the publication )

Lab Invest, 2019, 99(11):1636-1649

PubMed: 31249375 ( click the link to review the publication )

Biosci Rep, 2019, 39(8)

PubMed: 31316001 ( click the link to review the publication )

Clin Transl Oncol, 2019,

PubMed: 30632010 ( click the link to review the publication )

Nephron, 2019, 10.1159/000499506

PubMed: 31048591 ( click the link to review the publication )

Phytomedicine, 2019, 61:152859

PubMed: 31039534 ( click the link to review the publication )

Nat Commun, 2018, 9(1):3825

PubMed: 30237420 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(17):4162-4174

PubMed: 29776956 ( click the link to review the publication )

Molecules, 2018, 23(11)E2918

PubMed: 30413113 ( click the link to review the publication )
PLoS One, 2018, 13(10-:e0204930

PubMed: 30281669 ( click the link to review the publication )

Connect Tissue Res, 2018, 59(2):108-119

PubMed: 28301220 ( click the link to review the publication )

J Clin Invest, 2017, 127(10):3624-3639

PubMed: 28846069 ( click the link to review the publication )

Nat Commun, 2017, 8:14348

PubMed: 28128308 ( click the link to review the publication )

J Cell Sci, 2017, 130(18):2971-2983

PubMed: 28754687 ( click the link to review the publication )

Sci Rep, 2017, 7(1):5765

PubMed: 28720870 ( click the link to review the publication )

Radiat Res, 2017, 187(1):79-88

PubMed: 28001908 ( click the link to review the publication )

Int J Clin Exp Pathol, 2017, 10(8):8324-8333

PubMed: 31966683 ( click the link to review the publication )

Cancer Res, 2016, 76(12):3484-95

PubMed: 27216180 ( click the link to review the publication )

Cancer Discov, 2016,

PubMed: 26811325 ( click the link to review the publication )

Mol Cancer Ther, 2016, 15(12):2916-2925

PubMed: 27638856 ( click the link to review the publication )

Lab Invest, 2016, 96(11):1178-1188

PubMed: 27668890 ( click the link to review the publication )

Mol Carcinog, 2016, 10.1002/mc.22587

PubMed: 27805285 ( click the link to review the publication )

Mol Biol Cell, 2016, 27(20):3085-3094

PubMed: 27559126 ( click the link to review the publication )

Onco Targets Ther, 2016, 9:1415-23

PubMed: 27042110 ( click the link to review the publication )

Oncotarget, 2016, 7(4):4680-94

PubMed: 26717039 ( click the link to review the publication )

Sci Rep, 2016, 6:35347

PubMed: 27734947 ( click the link to review the publication )

J Clin Invest, 2015, 10.1172/JCI79327

PubMed: 25822023 ( click the link to review the publication )

Biomaterials, 2015, 64:33-44

PubMed: 26115412 ( click the link to review the publication )

Cell Rep, 2015, 13(3):599-609

PubMed: 26456826 ( click the link to review the publication )

Biochim Biophys Acta, 2015, 1853(10 Pt A):2610-20

PubMed: 26193076 ( click the link to review the publication )

Oncotarget, 2015, 6(26):22239-57

PubMed: 26068949 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Integrin Inhibitors

Biological Activity

Description

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	NX3PdXdPTnWwY4Tpc44hSXO\|YYm=	Mn[xOVAh\|rypL33s	MX:zNE83OC9zMkCgcYlv		NGj2cIFqdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhTkGNLDDTdoMh[W6mIFHreC=>	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
HMEC-1	M4XmeGZ2dmO2aX;uJGF{e2G7	MmiwNlAwPDBxNkCg{txoN22u			MkTJbY5pcWKrdIOgSmFMKGGwZDDTdoPDqA>?	NYrFW29RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
G44	NUThRVlRSXCxcITvd4l{KEG\|c3H5	M3HselEwPS93MDFOwIcwdWx?	M3rUPVI1KGh?		NWPUfY9FcW6mdXPld{BieG:ydH;zbZM>	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
G28	NVzIVIhESXCxcITvd4l{KEG\|c3H5	NFXEO4kyNzVxNUCg{txoN22u	NUHCVFRIOjRiaB?=		MnzKbY5lfWOnczDhdI9xfG:\|aYO=	NY\xTFdrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxNVQxODVpPkG5NVE1ODB3PD;hQi=>
G44	MXzQdo9tcW[ncnH0bY9vKEG\|c3H5	M1zh[VEwPS93MDFOwIcwdWx?	NV25ZXQ5OjRxNEivO\|IhcA>?		NEXMRpNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	NHPGTFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
G28	NITH[WRRem:uaX\ldoF1cW:wIFHzd4F6	NGroR3oyNzVxNUCg{txoN22u	NYe4OphROjRxNEivO\|IhcA>?		M2PTbYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	NGK4SZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1	NHPORWVCeG:ydH;zbZMhSXO\|YYm=	NHfTS2gyNzVxNUCg{txoN22u	NYTmOodFOjRiaB?=		M3HKU4lv\HWlZYOgZZBweHSxc3nz	NGT3e4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUGxOFAxPSd-MUmxNVQxODV:L3G+
HMEC-1	MV3Qdo9tcW[ncnH0bY9vKEG\|c3H5	NH\LXFAyNzVxNUCg{txoN22u	MorVNlQwPDhxN{KgbC=>		MWPpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz	M1fOPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUG0NFA2Lz5zOUGxOFAxPTxxYU6=
HMEC-1	MYjGeY5kfGmxbjDBd5NigQ>?	M33KT\|EwPS93MDFOwIcwdWx?	MmTqNlQhcA>?		MkG4bY5lfWOnczDhJIRwe2ViZHXw[Y5l\W62IHTleIFkcG2nboVCpC=>	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTFzNECwOUc,OTlzMUSwNFU9N2F-
LNT-229	NETpfVVHfW6ldHnvckBCe3OjeR?=	NYW3TJJCOC5zL{GvNVAh\|ryP	NXrlVGJROjRiaB?=		NFuybJFqdXCjaYLzJJRp\SCjZHjld4lwdiCxZjDj[YxteyC2bzD2bZRzd26nY4TpckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=>	MoHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO\|EoRjF7MkKxNVcyRC:jPh?=
T98G	M16yNmZ2dmO2aX;uJGF{e2G7	MorENE4yNzFxMUCg{txO	MVOyOEBp		NUnnfXpLcW2yYXnyd{B1cGViYXTo[ZNqd25ib3[gZ4VtdHNidH:geol1em:wZXP0bY4hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI>	MmD5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO\|EoRjF7MkKxNVcyRC:jPh?=
LN-18	MX\GeY5kfGmxbjDBd5NigQ>?	NGPHPGwxNjFxMT:xNEDPxE1?	M33KTFI1KGh?		MkD6bY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	Ml7QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MkGxO\|EoRjF7MkKxNVcyRC:jPh?=
LN-308	NGG1dnZHfW6ldHnvckBCe3OjeR?=	MnrWNE4yNzFxMUCg{txO	M1XtTFI1KGh?		MnW1bY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	NEPRZXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKyNVE4OSd-MUmyNlEyPzF:L3G+
U87MG	MWDGeY5kfGmxbjDBd5NigQ>?	NXLlWnB3OC5zL{GvNVAh\|ryP	NYDjcpRxOjRiaB?=		MoXFbY1x[Wm{czD0bIUh[WSqZYPpc44hd2ZiY3XscJMhfG9idnn0do9v\WO2aX6gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	M3jRTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkKxNVcyLz5zOUKyNVE4OTxxYU6=
U87	NILlW45HfW6ldHnvckBCe3OjeR?=	NUjQS5Z5OC1{NTFOwIcwdUx?	MVOxNkBpyqB?		MV\pcoR2[2W\|IHH1eI9xcGGpeTDkc5NmKGSncHXu[IVvfGy7	MkTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N\|Q{RC:jPh?=
U251	MlHHSpVv[3Srb36gRZN{[Xl?	M3:4WlAuOjVizsznM41N	M3LKN\|EzKGkEoB?=		M2nMfYlv\HWlZYOgZZV1d3CqYXf5JIRwe2ViZHXw[Y5l\W62bIm=	M{C3dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N\|Q{Lz5{MUe4PFM1OzxxYU6=
U87	NEHmZVRCeG:ydH;zbZMhSXO\|YYm=	NXrXNXBkOjVizsznM41N	MYqyOE81QCCq		M2XyWYlv\HWlZYOgZZBweHSxc3nzJIF1KDR6IHigd4lodmmoaXPhcpRtgQ>?	Mk\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OEizOFMoRjJzN{i4N\|Q{RC:jPh?=
U251	MYfBdI9xfG:\|aYOgRZN{[Xl?	M3jZR\|I2KM7:Zz;tUC=>	Mk[wNlQwPDhiaB?=		M4\RSYlv\HWlZYOgZZBweHSxc3nzJIF1KDR6IHigd4lodmmoaXPhcpRtgQ>?	NFz6NnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe4PFM1Oyd-MkG3PFg{PDN:L3G+
U87	NXL1[Y1lT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3XTU\|AuOjVizsznM41N	Ml6wNE01QCCq		MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK=	M4f4VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{i4N\|Q{Lz5{MUe4PFM1OzxxYU6=
U251	NVPSeFF7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvCNE0zPSEQvHevcWw>	NV;Xd5k{OC12ODDo		NV33OJMzcW6qaXLpeJMh[2WubDDndo94fGhiaX6g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd6OEO0N{c,OjF5OEizOFM9N2F-
U251MG	MVTBdI9xfG:\|aYOgRZN{[Xl?	NF3uRYwyKML3TR?=	NFHJXW81QCCq		NGjXTVlqdmS3Y3XzJIFxd3C2b4Ppdy=>	MkHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|NUS4NFcoRjJ\|M{W0PFA4RC:jPh?=
U87MG	MVnBdI9xfG:\|aYOgRZN{[Xl?	NGPlXZMyKML3TR?=	NHX3VIQ1QCCq		NVqwbppycW6mdXPld{BieG:ydH;zbZM>	NEPs[pg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OFgxPyd-MkOzOVQ5ODd:L3G+
U251MG	NV7y[pZRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoTyNE0zPSEQvF2=	M4jLcVI1NzR6IHi=		MnXnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy	Mlm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|NUS4NFcoRjJ\|M{W0PFA4RC:jPh?=
U87MG	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUCwXJF5OC1{NTFOwG0>	NWHjPGJFOjRxNEigbC=>		MV;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK=	M3\WPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{W0PFA4Lz5{M{O1OFgxPzxxYU6=
MCF-7	MXPBdI9xfG:\|aYOgRZN{[Xl?	M3jFN\|AuOjBizszN	M3\VV\|Q5KGh?		MknQbY5lfWOnczDhdI9xfG:\|aYO=	MmXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOxNFIoRjJ2MUWzNVAzRC:jPh?=
T-47D	NEPGWIVCeG:ydH;zbZMhSXO\|YYm=	MWKwMVIxKM7:TR?=	NFrOeWg1QCCq		NGm0TVZqdmS3Y3XzJIFxd3C2b4Ppdy=>	NVnQb3ZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMyODJpPkK0NVU{OTB{PD;hQi=>
MCF-7	NYXFU3dsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmTrNE0zOCEQvF2=	NUHkOGl2QTZiaB?=		NUn6[2s5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	NVvKOY5ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMyODJpPkK0NVU{OTB{PD;hQi=>
T-47D	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV6wMVIxKM7:TR?=	MnryPVYhcA>?		NIP4dmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	M1PRO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUWzNVAzLz5{NEG1N\|ExOjxxYU6=
FaDu	MX\BdI9xfG:\|aYOgRZN{[Xl?	NFHqTVczPcLiwsXNxsA>	MW[0POKhcMLi		NGT4UmNqdmS3Y3XzJIFxd3C2b4Ppdy=>	NWrie\|B[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
CAL27	MX\BdI9xfG:\|aYOgRZN{[Xl?	MljtNlXDqML3TdMg	MX60POKhcMLi		MX7pcoR2[2W\|IHHwc5B1d3Orcx?=	NXLOS4RXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OVcxPTZpPkK0OVU4ODV4PD;hQi=>
SCC25	M175XGFxd3C2b4Ppd{BCe3OjeR?=	MYeyOeKhyrWPwrC=	MUO0POKhcMLi		Mln2bY5lfWOnczDhdI9xfG:\|aYO=	NFnsPFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW1O\|A2Pid-MkS1OVcxPTZ:L3G+
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U87MG	M2r2b2FvfGlvaX72ZZNqfmViYYPzZZk>	MXexNEB2VQ>?	MknTNlQhcHK\|		MoG3RY51cS2rbo\hd4l3\SCjY4Tpeol1gSCrbjDoeY1idiCXOEfNS{Bk\WyuczDheEAyOCC3TTDh[pRmeiB{NDDodpMh[nlidILhcpN4\WyuIHHzd4F6	Mlj4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5N{WzNFMoRjJ7N{e1N\|A{RC:jPh?=
U87MG	MlfBRY51cS2rbo\hd4l3\SCjc4PhfS=>	NXTZemZFOTBidV2=	MlPpNlQhcHK\|		MVPBcpRqNWmwdnHzbZZmKGGldHn2bZR6KGmwIHj1cYFvKFV6N13HJINmdGy\|IHH0JFExKHWPIHHmeIVzKDJ2IHjyd{BqdiCycnXz[Y5k\SCxZjDNSG0zKGmwaHnibZRweiCwdYTsbY4uOyCjbnSgUWROPCCrbnjpZol1d3JiU1qtNVczOjV3MDDifUB1emGwc4flcIwh[XO\|YYm=	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd5NUOwN{c,Ojl5N{WzNFM9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pFAK / p-AKT ; PubMed: 19114005 J Exp Clin Cancer Res 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 Cell Death Dis 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 PLoS One 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 Radiat Oncol 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

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

Kinase Assay:^[2]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: Human glioblastoma xenografts U87 MG Dosages: 100μg Administration: Daily i.p. (Only for Reference)

References

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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 Download Cilengitide trifluoroacetate SDF

Molecular Weight	702.68
Formula	C₂₉H₄₁F₃N₈O₉
CAS No.	199807-35-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	EMD 121974, NSC 707544
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

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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.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

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

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

Tel: +1-832-582-8158 Ext:3

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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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Cilengitide trifluoroacetate