PTC-209 |
Catalog No.GC15725 |
PTC-209, un composé de faible poids moléculaire qui inhibe sélectivement BMI-1 avec une IC50 de 0,5 µM dans les cellules HT1080, est un anticancéreux prometteur.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 315704-66-6
Sample solution is provided at 25 µL, 10mM.
PTC-209, a low-molecular-weight compound that selectively inhibits BMI-1 with IC50 for 0.5µM in HT1080 cells, is a promising anticancer[1,2]
In vitro, PTC-209 treats human colorectal cancer cells with doses between 0.1 and 10µM reduced BMI-1 protein levels in a dose-dependent manner with a concomitant reduction in cell growth[1]. PTC-209 causes a concentration- and time-dependent decrease in the cellular viability of lung cancer cells (LNM35 and A549), breast cancer cells (MDA-MB-231 and T47D), and colon cancer cells (HT-29, HCT8/S11, and HCT-116)[2]. Treatment with PTC-209 significantly decreased viable cell numbers in human multiple myeloma (MM) cell lines, induced a G1 cell cycle arrest, promoted apoptosis and demonstrated synergistic activity with pomalidomide and carfilzomib. In the MM microenvironment, PTC-209 impaired tube formation, impaired osteoclast development and decreased osteoblast formation in a dose-dependent manner (P < 0.01 at 1μM, respectively). Therapeutic targeting of BMI-1 by PTC-209 is a promising novel therapeutic intervention for MM[3]
PTC-209 combined with palbociclib inhibit tumor cell proliferation, sphere and colony formation, migration, and in vivo tumor formation[4]. PTC-209 administration significantly reduced tumor growth in a HNSCC xenograft model by Bmi1 inhibition and impaired cell proliferation in vivo[5]. PTC-209 significantly attenuates the glioblastoma growth in a murine orthotopic xenograft model[6]
References:
[1].Kreso A, van Galen P, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014;20(1):29-36.
[2].Sulaiman S, Arafat K, et al. PTC-209 Anti-Cancer Effects Involved the Inhibition of STAT3 Phosphorylation. Front Pharmacol. 2019;10:1199. Published 2019 Oct 21.
[3].Bolomsky A, Schlangen K, et al. Targeting of BMI-1 with PTC-209 shows potent anti-myeloma activity and impairs the tumour microenvironment. J Hematol Oncol. 2016;9:17. Published 2016 Mar 2.
[4]. Elango R, Vishnubalaji R, et al. Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo. Sci Rep. 2019;9(1):13696. Published 2019 Sep 23.
[5].Wang Q, Li Z, et al. Pharmacological inhibition of Bmi1 by PTC-209 impaired tumor growth in head neck squamous cell carcinoma. Cancer Cell Int. 2017;17:107. Published 2017 Nov 21.
[6].Kong Y, Ai C, et al. Targeting of BMI-1 with PTC-209 inhibits glioblastoma development. Cell Cycle. 2018;17(10):1199-1211
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