For research use only. Not for therapeutic Use.
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models[1][2][3].
RGD-4C (2.5, 5, 10 μg/mL) inhibits BAE cell proliferation by synthetic form modified with endostatin-derived peptides[2].
RGD-4C (9.11 mg/kg; injection; single dose) inhibits the growth of B16F10 mouse melanoma in vivo[2].
Modified RGD-4C fused with the N-terminus of plant-derived single-chain ribosome inactivating protein saporin (SAP) (called RGD-SAP), (diluted in sodium chloride, 0.9%; i.v.; 200 µL; every 5 days, for 3 times) exerts anti-tumor activity in a model of muscle invasive bladder cancer[3].
RGD-SAP in combination with mitomycin C, a chemotherapeutic drug, increases the survival of mice bearing orthotopic bladder cancer with no evidence of systemic toxicity[3].
| Catalog Number | I042534 |
| CAS Number | 332179-76-7 |
| Synonyms | 2-[(1R,4S,7R,12R,15S,18R,21S,27S)-7-[[(2S)-2-aminopropanoyl]amino]-15-benzyl-4-(carboxymethyl)-12-(carboxymethylcarbamoyl)-27-[3-(diaminomethylideneamino)propyl]-3,6,14,17,20,23,26,29-octaoxo-9,10,31,32-tetrathia-2,5,13,16,19,22,25,28-octazabicyclo[16.11.4]tritriacontan-21-yl]acetic acid |
| Molecular Formula | C42H60N14O16S4 |
| Purity | ≥95% |
| InChI | InChI=1S/C42H60N14O16S4/c1-19(43)33(64)53-26-16-74-73-15-25(35(66)48-14-32(62)63)54-36(67)22(10-20-6-3-2-4-7-20)51-41(72)28-18-76-75-17-27(56-38(69)24(12-31(60)61)52-40(26)71)39(70)50-21(8-5-9-46-42(44)45)34(65)47-13-29(57)49-23(11-30(58)59)37(68)55-28/h2-4,6-7,19,21-28H,5,8-18,43H2,1H3,(H,47,65)(H,48,66)(H,49,57)(H,50,70)(H,51,72)(H,52,71)(H,53,64)(H,54,67)(H,55,68)(H,56,69)(H,58,59)(H,60,61)(H,62,63)(H4,44,45,46)/t19-,21-,22-,23-,24-,25-,26-,27-,28-/m0/s1 |
| InChIKey | DXIKEERYADAVLF-CFFDDJBSSA-N |
| SMILES | CC(C(=O)NC1CSSCC(NC(=O)C(NC(=O)C2CSSCC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)N2)CC(=O)O)CCCN=C(N)N)NC(=O)C(NC1=O)CC(=O)O)CC3=CC=CC=C3)C(=O)NCC(=O)O)N |
| Reference | [1]. Assa-Munt N, et al. Solution structures and integrin binding activities of an RGD peptide with two isomers. Biochemistry. 2001 Feb 27;40(8):2373-8. [2]. Yin R, et al. Effect of RGD-4C position is more important than disulfide bonds on antiangiogenic activity of RGD-4C modified endostatin derived synthetic polypeptide. Bioconjug Chem. 2010 Jul 21;21(7):1142-7. [3]. Zuppone S, et al. A Novel RGD-4C-Saporin Conjugate Inhibits Tumor Growth in Mouse Models of Bladder Cancer. Front Oncol. 2022 Apr 11;12:846958. |
