CTB006 

CTB006 is a monoclonal antibody targeting a humanized chimeric recombinant anti-DR5. CTB006 specifically binds to and activates DR5, thereby inducing tumor cell apoptosis, inhibiting tumor growth and reducing tumor drug resistance. ¹⁷⁷Lu-radiolabeled CTB006 can deliver targeted radiotherapy to tumor cells; while ⁸⁹Zr- or ¹⁷⁷Lu-labeled CTB006 can serve as a PET/CT imaging agent for detecting DR5 expression levels in preclinical tumor models and screening cancers with DR5 overexpression. CTB006 can be applied to research related to gastrointestinal cancer, colorectal cancer and other solid tumors^[1][2][3].

Human

The combination of DR5 agonist monoclonal antibody CTB-006 and IAP antagonist APG-1387 exhibits strong anti-tumor activity in MDA-MB-231 and 2LMP TNBC human breast cancer cell lines^[1].
⁸⁹Zr-CTB006 (4 µg/mL; 1 hour) binds with highest affinity to DR5-positive Colo205 cells, with a dissociation constant of 65.24 nmol^[2].
¹⁷⁷Lu-DOTA-CTB006 (0.015-32 nM; 1 h) binds specifically to colo205 cells with an EC₅₀ of 2.919 nM and a K_d of 4.24 nM^[3].
Unlabeled DOTA-CTB006 (0.06-400 nM; 1 h) competes with ¹⁷⁷Lu-DOTA-CTB006 for binding to colo205 cells with an IC₅₀ of 8.78 nM^[3].

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

⁸⁹Zr-CTB006 (5.18 MBq; parenteral) exhibits a characteristic biodistribution pattern in healthy female Balb/c mice, with high initial uptake in blood and reticuloendothelial organs and gradual marrow accumulation^[2].
⁸⁹Zr-CTB006 (3.7 MBq; i.v.; single dose) specifically accumulates in DR5-positive Colo205 xenografts, with peak tumor uptake of 12.75 %ID/g at 168 hours post-injection^[2].
¹⁷⁷Lu-DOTA-CTB006 (1.5 mg/kg; i.v.; single dose) produces significant colorectal tumor growth inhibition in BALB/c mice with colo205 xenografts, resulting in an average relative tumor volume of 1.775 after 29 days^[3].
⁸⁹Zr-DFO-CTB006 (1.85 MBq; i.v.; single dose) exhibits high, long-lasting uptake in colo205 xenografts in BALB/c mice, reaching a maximum of 5.45 % ID/g at 168 h^[3].
¹⁷⁷Lu-DOTA-CTB006 (0.74 MBq; i.v.; single dose) accumulates increasingly in colo205 xenografts in BALB/c mice, reaching 8.29% ID/g at 168 h, exceeding liver accumulation at this time point^[3].

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

8795  [NCBI]

O14763

TNFRSF10B/TRAILR2/CD262

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gamie Z, et al. Targeting Death Receptor 5 (DR5) for the imaging and treatment of primary bone and soft tissue tumors: an update of the literature. Front Mol Biosci. 2024;11:1384795. Published 2024 Sep 2.

  [2]. Wang S, et al. First-in-human DR5 PET reveals insufficient DR5 expression in patients with gastrointestinal cancer. J Immunother Cancer. 2021;9(7):e002926.

  [3]. Yang Y, et al. 89Zr and 177Lu labeling of anti-DR5 monoclonal antibody for colorectal cancer targeting PET-imaging and radiotherapy[J]. Journal of Radioanalytical and Nuclear Chemistry, 2021, 330(3): 997-1005.