925681-61-4
Chemical Structure
Trabedersen
Synonym(s): AP 12009
- CAS No.: 925681-61-4
- Formula:N/A
- Molecular Weight:5768.70
IUPAC Name: 3-fluoro-5-(((1S,2S)-2-fluoro-1-hydroxy-7-(methylsulfonyl)-3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)benzonitrile
SMILES: [Trabedersen]
Biological Activity: Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma[1][2][3][4].
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Trabedersen | 91.24% | Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma. | ||||||||||||||||||||
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- [1]. Vallières L. Trabedersen, a TGFbeta2-specific antisense oligonucleotide for the treatment of malignant gliomas and other tumors overexpressing TGFbeta2[J]. IDrugs, 2009, 12(7): 445-453.
- [2]. Rothhammer-Hampl T, et al. Targeted suppression of TGF-beta2 by trabedersen (AP 12009) in an orthotopic xenograft melanoma mouse model[J]. Cancer Research, 2012, 72(8_Supplement): 2362-2362.
- [3]. Schlingensiepen KH, et al. Transforming growth factor-beta 2 gene silencing with trabedersen (AP 12009) in pancreatic cancer. Cancer Sci. 2011;102(6):1193-1200. [Content Brief]
- [4]. Bogdahn U, et al. Targeted therapy for high-grade glioma with the TGF-β2 inhibitor trabedersen: results of a randomized and controlled phase IIb study. Neuro Oncol. 2011;13(1):132-142. [Content Brief]
Keywords
