hIMB1636
hIMB1636 is a humanized monoclonal antibody targeting Trop2. By binding to the conformational Trop2 epitope, hIMB1636 regulates related signaling pathways, triggers lysosomal endocytosis, and further induces apoptosis, cell cycle arrest, and antibody-dependent cellular cytotoxicity. hIMB1636 effectively inhibits tumor cell proliferation, migration and in vivo tumor growth, and also exerts bystander killing effect and mediates long-term retention. hIMB1636 can be conjugated with NOTA/DOTA for radiolabeling to enable immuno-PET imaging, or prepared as hIMB1636-LDP-AE to significantly inhibit the growth of breast cancer and lung cancer xenografts.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Human
hIMB1636 (1.56-50 nM) binds to recombinant human Trop2 protein with a Kd of 0.603 nM[1].
hIMB1636 (5-10 μM; 72 h) potently inhibits proliferation of MDA-MB-468 and MDA-MB-231 cells in a Trop2-dependent manner, with superior activity compared to sacituzumab[2].
hIMB1636 (5-10 μM; 36 h (MDA-MB-468); 12 h (MDA-MB-231)) inhibits migration of MDA-MB-468 and MDA-MB-231 cells in a Trop2-dependent manner[2].
hIMB1636 (5 μM; 24 h) induces caspase-dependent apoptosis in MDA-MB-468 and MDA-MB-231 cells by upregulating cleaved caspase-9, cleaved caspase-3, and cleaved PARP[2].
hIMB1636 (5 μM; 24 h) significantly increases the proportion of apoptotic cells in MDA-MB-468 and MDA-MB-231 cells[2].
hIMB1636 binds specifically to T3M-4 pancreatic cancer cells, which show the highest Trop2 expression among tested pancreatic cancer cell lines, as confirmed by multiple cell-based binding assays[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, MDA-MB-231
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Concentration:5 μM, 10 μM
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Incubation Time:72 h
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Result:Inhibited cell proliferation in a dose-dependent manner in MDA-MB-468 cells, with 10 μM hIMB1636 reducing proliferation to 22.60% of control levels.
Reduced proliferation to ~15% of control levels in MDA-MB-231 cells at both 5 μM and 10 μM, indicating saturation of surface Trop2 at the lower concentration.
Exhibited significantly stronger proliferation inhibition than sacituzumab at matching concentrations in both cell lines.
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Cell Line:MDA-MB-468, MDA-MB-231
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Concentration:5 μM
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Incubation Time:24 h
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Result:Reduced expression of cyclin D1 and CDK6, and increased expression of P21, compared to control cells.\nUpregulated expression of cleaved caspase-9, cleaved caspase-3, and cleaved PARP, indicating activation of the caspase-dependent apoptotic pathway.
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Cell Line:MDA-MB-468, MDA-MB-231
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Concentration:5 μM
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Incubation Time:24 h
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Result:Significantly increased the ratio of early and late apoptotic cells in both cell lines, with MDA-MB-468 cells showing an increase from 8.25% to 12.89% apoptotic cells, and MDA-MB-231 cells showing an increase from 3.70% to 11.05% apoptotic cells.
hIMB1636 (25-50 mg/kg; i.v.; every 5 days; 4 total doses) exhibits potent in vivo antitumor activity in MDA-MB-468 xenografts, achieving tumor inhibition rates of 61.4% at 50 mg/kg and 58.2% at 25 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (6-week-old female; HCC827 cells injected subcutaneously into right flank)[1]
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Dosage:0.8 mg/kg
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Administration:i.v.; every five days; 4 total injections
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Result:Showed no antitumor effects, with tumor volumes similar to that of the control group.
Caused no significant body weight loss.
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Animal Model:BALB/c nude (6-week-old female)[2]
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Dosage:50 mg/kg; 25 mg/kg
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Administration:i.v.; every 5 days; 4 total doses
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Result:Produced a tumor inhibition rate of 61.4% at 50 mg/kg on day 37 post-tumor implantation.
Produced a tumor inhibition rate of 58.2% at 25 mg/kg on day 37 post-tumor implantation.
Caused no significant weight loss.
TROP2
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]. Zhou DD, et al. A new TROP2-targeting antibody-drug conjugate shows potent antitumor efficacy in breast and lung cancers. NPJ Precis Oncol. 2024;8(1):94. Published 2024 Apr 23. [Content Brief]
[2]. Zhou DD, et al. Elucidating the development, characterization, and antitumor potential of a novel humanized antibody against Trop2. Int J Biol Macromol. 2023;253(Pt 6):127105. [Content Brief]
[3]. Duan H, et al. Advances and Prospects in the Treatment of Pancreatic Cancer. Int J Nanomedicine. 2023;18:3973-3988. Published 2023 Jul 19. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
hIMB1636 Related Classifications
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