Cilengitide, EMD 121974
General Information
DRACP ID DRACP02537
Peptide Name Cilengitide, EMD 121974
Sequence RGDfX
Sequence Length 5
UniProt ID Not available
PubChem CID 176873
Origin RGD Fibronectin
Type Synthetic peptide
Classification
Active ACP Cancer targeted peptides Antiangiogenic Inhibitor of the integrins ανβ3 and ανβ5
Activity Information
Cell Line | Disease | Cancer Classified | Activity | Assay | Testing Time | Literature |
---|---|---|---|---|---|---|
M21 | Melanoma | Carcinoma | IC50 (Cilengitide inhibited integrin-mediated binding to vitronectin) =0.4 µM | Lysosomal hexosaminidase quantitative assay | Not available | 1 |
UCLA-P3 | Lung squamous cell carcinoma | Carcinoma | IC50 (Cilengitide inhibited integrin-mediated binding to vitronectin) =0.4 µM | Lysosomal hexosaminidase quantitative assay | Not available | 1 |
Hemolytic Activity Not available
Normal (non-cancerous) Cytotoxicity Not available
Target Integrins αvβ3, αvβ5
Affinity Not available
Mechanism Not available
Nature Anticancer
Structure Information
Helicity Not available
Linear/Cyclic Cyclic
Disulfide/Other Bond NCB: Arg1<--->X5
N-terminal Modification Free
C-terminal Modification Free
Other Modification f=D-Phe
Chiral Mix
Physicochemical Information
Formula C12H18N6O4
Absent amino acids ACEFHIKLMNPQSTVWY
Common amino acids DGRX
Mass 49184
Pl 6.34
Basic residues 1
Acidic residues 1
Hydrophobic residues 0
Net charge 0
Boman Index -2270
Hydrophobicity -168
Aliphatic Index 0
Half Life
/
Extinction Coefficient cystines 0
Absorbance 280nm 0
Polar residues 1
Amino acid distribution
Literature Information
Literature 1
Pubmed ID 11855984
Title Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins
Year 2002
Patent
Patent ID Not available
Patent Title Not available
Other Iinformation Not available
Other Published ID Not available