3BP-3940 

3BP-3940 is a highly potent and selective peptide inhibitor of FAP that targets cancer-associated fibroblasts (CAFs) in the tumor microenvironment. 3BP-3940 can be labeled with radionuclides (such as Ga-68) for precise tumor imaging or Lu-177 for the development of targeted anticancer technologies. 3BP-3940 accumulates in tumor lesions and can be used to diagnose and inhibit various solid cancers and CAFs-related diseases^[1][2].

3BP-3940 (50 μg; radiolabeling with Ga-68) + In the automated radiolabeling process of ^[??Ga]Ga-3BP-3940, using 50 μg of 3BP-3940 in a total of 7 mL labeling volume with sodium acetate buffer (0.7 M, pH 5.5, 2 mL) at 85°C, provides decay-corrected radiochemical yields (RCY’s) of ≥90% within 20 min, and the automated synthesis yields activities of the final drug product between 308 MBq and 987 MBq (decay corrected RCY = 93.1 ± 5.7%)， with a radiochemical purity (RCP) of ≥97% in process validation and a mean RCP of 97.7±0.9% in subsequent routine productions^[1]. 3BP-3940 (37-50 mg/GBq; radiolabeling with Lu-177) + In the automated radiolabeling process of ^[1??Lu]Lu-3BP-3940, using 37-50 mg of 3BP-3940 per GBq with a 0.1 M ascorbic acid solution containing gentisic acid (1.2 mL, pH 4.5, 30 mg gentisic acid) at 85°C for 30 min, gives high RCY results. The average RCP of the process validation runs is 97.5 ± 1.4% and the average yield is 94.4 ± 1.6%, and in subsequent routine productions, a mean RCP of 96.8±1.2% and a mean RCY of 91.5±9.1% at the end of synthesis are observed^[1]. 3BP-3940 (not specified in terms of concentration; in vitro stability test) + Both ^[??Ga]Ga-3BP-3940 and ^[1??Lu]Lu-3BP-3940 show no significant release of the radiometal over the course of two half-lives of the corresponding isotopes when incubated in human serum (HS) and saline (NaCl) at 37°C, with a complex stability of >90% under both conditions, and the RCP of both compounds is >95% 2 h after formulation as determined by HPLC^[1]. 3BP-3940 (0.5-10 mg/mL for UV detection, 0.1-1.0 MBq for radioactivity detection; HPLC method validation) + In the HPLC method validation for ^[??Ga]Ga-3BP-3940, linearity, accuracy, precision, specificity, lower limit of detection (LLOD)， and lower limit of quantification (LLOQ) meet the requirements of the ICH guideline Q2 and the EANM guideline on validation. For example, in linearity (UV detection)， with seven different concentrations of ^[???Ga]Ga-3BP-3940 (0.5-10 mg/mL)， the R2 of the regression line is above 0.998 and relative standard deviations (RSD) <2%; in accuracy (radioactivity detection)， nine different measurements at nine different Ga-68 radioactivity concentration levels in the range of 75%-368% have an average recovery of 100.5% with an RSD of 0.5%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1471.76

C₆₆H₉₈N₁₄O₁₈S₃

2803421-14-7

Solid

White to off-white

nBu-CAyl-{Cys(tMeBn(DOTA-AET)-Pro-Pro-Thr-GIn-Phe-Cys}-OH

nBu-CAyl-{Cys(tMeBn(DOTA-AET)-PPTQFC}-OH

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Greifenstein L, et al. 3BP-3940, a highly potent FAP-targeting peptide for theranostics-production, validation and first in human experience with Ga-68 and Lu-177. iScience. 2023 Nov 23;26 (12) :108541.  [Content Brief]

  [2]. Kramer C S, et al. FAP-Peptidvermittelte Radiorezeptortherapie (PTRT) bei soliden Tumoren: erste klinische Erfahrungen mit dem 177Lu-, 225Ac-oder 90Y-markierten Peptid 3BP-3940^[J]. Nuklearmedizin-NuclearMedicine, 2023, 62 (02) : V14.