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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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 Kd 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 (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.
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Animal Model:BALB/c (16-20 g, subcutaneous inoculation of 3×106 colo205 cells, tumor size 0.3-0.5 cm3)[3]
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Dosage:1.5 mg/kg equivalent antibody dose (7.4 MBq total radioactivity)
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Administration:i.v.; single dose
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Result:Inhibited tumor growth significantly in all 5 treated mice over 29 days, with an average relative tumor volume (RTV) of 1.775 at the end of the experiment.
Showed no obvious liver lesions in histological analysis.
Demonstrated significantly different anti-tumor efficacy (P < 0.01) compared to control groups treated with saline or unlabeled CTB006 at the same 1.5 mg/kg dose.
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Animal Model:BALB/c (16-20 g, subcutaneous inoculation of 3×106 colo205 cells, tumor size 0.3-0.5 cm3)[3]
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Dosage:1.85 MBq (specific activity 63 MBq/mg)
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Administration:i.v.; single dose
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Result:Achieved visible tumor uptake at 24 h that persisted for 312 h.
Reached maximum tumor uptake of 5.45 % ID/g at 168 h.
Exceeded liver accumulation from 48 h onward and exceeded heart accumulation from 96 h onward.
Decreased liver accumulation from 4.9 % ID/g at 1 h to 2.15 % ID/g at 312 h.
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Animal Model:BALB/c (16-20 g, subcutaneous inoculation of 3×106 colo205 cells, tumor size 0.3-0.5 cm3)[3]
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Dosage:0.74 MBq (specific activity 246.7 MBq/mg)
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Administration:i.v.; single dose
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Result:Increased tumor uptake over time, from 2.85 % ID/g at 1 h to 8.29 % ID/g at 168 h.
Peaked liver uptake at 12.65 % ID/g at 24 h, which decreased to 6.53 % ID/g at 168 h.
Exceeded liver accumulation at 168 h.
TNFRSF10B/TRAILR2/CD262
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CTB006 Related Classifications
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