TROP2

EGP-1; M1S1; GA733-1

TROP2 is a transmembrane glycoprotein that belongs to the GA733 family. Trop2 has several ligands, including claudin-1, claudin-7, and cyclin D1. Trop2 activity requires regulated intramembrane proteolysis (RIP). RIP cleaves Trop2 by TNF-α converting enzyme (TACE), followed by γ-secretase cleavage within the transmembrane domain. TROP2 can activate the ERK1/3-MAPK pathway. TROP2 signals cells to self-renewal, proliferation, invasion, and survival. Trop2 has stem cell-like properties. TROP2 is overexpressed in a variety of human cancers, including breast, cervical, colorectal, esophageal (some types), lung (some types), non-Hodgkin lymphoma, chronic lymphocytic lymphoma (CLL), Rajburkitt's lymphoma, oral squamous cell carcinoma, ovarian, pancreatic, prostate, gastric, thyroid, bladder, and uterine cancers.

References:

[1]. Shvartsur A, et al. Trop2 and its overexpression in cancers: regulation and clinical/therapeutic implications. Genes Cancer. 2015 Mar;6(3-4):84-105. [Content Brief]

TROP2 Inhibitors (12)

TROP2 Related Products (12):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P99045

Sacituzumab	Inhibitor	99.9%
Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer.

HY-141598

Datopotamab deruxtecan (solution)	Inhibitor	99.98%
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 K_d of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer.

HY-132254

Sacituzumab govitecan	Inhibitor	99.13%
Sacituzumab govitecan (IMMU-132) is an antibody-drug conjugate (ADC) targeting Trop-2 for delivery of SN-38. The antibody portion is Sacituzumab (HY-P99045), and the drug-linker conjugate for ADC is CL2A-SN-38 (HY-128946). Sacituzumab govitecan shows anticancer activity.

HY-P99843

Datopotamab	Inhibitor	99.92%
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer.

HY-132254A

Sacituzumab govitecan (solution)	Inhibitor	99.19%
Sacituzumab govitecan (IMMU-132) is an antibody-drug conjugate (ADC) targeting Trop-2 for delivery of SN-38. The antibody portion is Sacituzumab (HY-P99045), and the drug-linker conjugate for ADC is CL2A-SN-38 (HY-128946). Sacituzumab govitecan shows anticancer activity.

HY-P992367

hIMB1636	Inhibitor
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.

HY-P992127

Renditatug	Inhibitor
Renditatug (BAT8008 Antibody) is an antibody targeting TROP2. Renditatug can be used for the synthesis of ADC BAT8008. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).

HY-164789

Sacituzumab tirumotecan	Inhibitor
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC₅₀ of 2.787 ng/ml, TROP2 K_a of 0.3083 nM, and topoisomerase I IC₅₀ of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer.

HY-P990827

Anti-TROP-2 Antibody (Pr1E11)	Inhibitor
Anti-TROP-2 Antibody (Pr1E11) is a kind of mouse IgG1 κ chimeric antibody inhibitor, targeting to human TROP-2. Anti-TROP-2 Antibody (Pr1E11) specifically binds to TROP-2 with high affinity and shows low internalization activitv. Anti-TROP-2 Antibody (Pr1E11) can be used for the research of cancer, such as epithelial cancer and primary pancreatic cancer.

HY-P991372

Anti-TROP2 Antibody	Inhibitor
Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody targeting Trop-2. Anti-TROP2 Antibody exerts in vitro inhibitory effects on a variety of tumor cell lines. Anti-TROP2 Antibody exhibits anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung PDX and triple-negative breast cancer (TNB) PDX models. Anti-TROP2 Antibody can be used for research on pancreatic cancer, ovarian cancer, lung cancer and triple-negative breast cancer.

HY-P99045A

Sacituzumab (powder)	Inhibitor	98.33%
Sacituzumab (powder) is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab (powder) demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab (powder) can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer.

HY-P991371

PF-06478924	Inhibitor
PF-06478924 (PF-06664178 antibody; RN926) is a human monoclonal antibody (mAb) targeting TROP2. PF-06478924 can be used in the study of advanced and metastatic solid tumors.

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