For research use only. Not for therapeutic Use.
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].
CEND-1 (iRGD) can modulate the solid tumour microenvironment, enhancing the delivery and therapeutic index of co-administered anti-cancer agents[4].
CEND-1 enhances the penetration of anticancer therapeutics specifically into tumours, but not into normal tissues, it also holds the potential for dose reductions, which can attenuate side effects[4].
CEND-1 (intravenously injected) increases the levels of co-administered Evans blue approximately threefold[5].
Table 1. Derived mean pharmacokinetic parameters for CEND-1 in mouse, rat, dog and monkey plasma after a single intravenous infusion of CEND-1 (±SD) [5].
Number of Animals (Sex)
CEND-1 Dose (mg/kg)
t1/2 (h)
C0 (ng/mL)
V (mL/kg)
Cl_obs (mL/hr/kg)
AUC0-inf (h*ng/mL)
Mouse *
3 (M)
1.5
0.306
10,343
449
1016
1476
3 (M)
13.5
0.547
68,358
1007
1277
10,569
Rat*
6 (M)
75
0.341
469,000
171
348
215,476
6 (F)
75
0.391
436,333
254
451
166,331
Dog*
3 (M)
1
0.665 (0.0448)
6010 (1985)
241 (27)
253 (40.1)
4030 (686)
3 (F)
5
0.648 (0.0486)
25,133 (3635)
230 (14.6)
247 (32.9)
20,443 (2530)
Monkey*
3 (M)
5
0.888 (0.0963)
55,082 (19,905)
204 (14.1)
179 (23.4)
28,230 (3865)
3 (M)
50
0.956 (0.0869)
602,161 (211,386)
162 (32.1)
178 (51.9)
421,119 (171,418)
Note:* Because of volume limitations in the mice and rats, each animal was used for one time point sampling, limiting the statistical analysis of the data. M, male; F, female.
| Catalog Number | I043271 |
| CAS Number | 2580154-02-3 |
| Synonyms | 2-[(6S,9S,15S,18R,23R,26S,29S)-18-acetamido-6-(4-aminobutyl)-23-carbamoyl-26-(carboxymethyl)-15-[3-(diaminomethylideneamino)propyl]-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-9-yl]acetic acid |
| Molecular Formula | C37H60N14O14S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C37H60N14O14S2/c1-18(52)45-24-17-67-66-16-23(30(39)59)50-34(63)22(13-29(57)58)49-36(65)25-8-5-11-51(25)27(54)15-44-32(61)19(6-2-3-9-38)47-33(62)21(12-28(55)56)46-26(53)14-43-31(60)20(48-35(24)64)7-4-10-42-37(40)41/h19-25H,2-17,38H2,1H3,(H2,39,59)(H,43,60)(H,44,61)(H,45,52)(H,46,53)(H,47,62)(H,48,64)(H,49,65)(H,50,63)(H,55,56)(H,57,58)(H4,40,41,42)/t19-,20-,21-,22-,23-,24-,25-/m0/s1 |
| InChIKey | YPHPUVJQSYACEN-HUVRVWIJSA-N |
| SMILES | CC(=O)NC1CSSCC(NC(=O)C(NC(=O)C2CCCN2C(=O)CNC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC1=O)CCCN=C(N)N)CC(=O)O)CCCCN)CC(=O)O)C(=O)N |
| Reference | [1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022 [2]. Ruoslahti Erkki, et al. Methods for treating pancreatic cancer and other solid tumors. WO2021226148. [3]. Andrew Peter Dean, et al. Updated single institution outcome data from the first-in-human CEND-1 trial in metastatic pancreatic cancer. Journal of Clinical Oncology 2021 39:15_suppl, e16274-e16274 [4]. Harri A Järveläinen, et al. Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1. Int J Mol Sci. 2023 Mar 16;24(6):5700. [5]. Schmithals, C, et al. Improving Drug Penetrability with iRGD Leverages the Therapeutic Response to Sorafenib and Doxorubicin in Hepatocellular Carcinoma. Cancer Res. 2015 Aug 1;75(15):3147-54. |
