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Certepetide

MCE China：Certepetide

Brand：MedChemExpress (MCE)

Cat. No.HY-P3448

CAS：2580154-02-3

Synonyms：CEND-1; iRGD; LSTA1

Purity：99.40%

Storage：Sealed storage, away from moisture and light, under nitrogen Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vivo：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.

IC50 & Target：Alphav-integrins, NRP-1[3]. In Vivo 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)

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References：

[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.  [Content Brief]

[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.  [Content Brief]