For research use only. Not for therapeutic Use.
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].
PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].
PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[2].
| Catalog Number | I000825 |
| CAS Number | 1217022-63-3 |
| Synonyms | N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-1,3-thiazol-2-amine;hydrobromide |
| Molecular Formula | C17H14Br3N5OS |
| Purity | ≥95% |
| InChI | InChI=1S/C17H13Br2N5OS.BrH/c1-9-15(24-5-3-4-20-16(24)21-9)13-8-26-17(22-13)23-14-11(18)6-10(25-2)7-12(14)19;/h3-8H,1-2H3,(H,22,23);1H |
| InChIKey | UOPFJYYKFDZXSY-UHFFFAOYSA-N |
| SMILES | CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br.Br |
| Reference | [1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36. [2]. Christian Mayr, et al. The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Oncotarget. 2016 Jan 5; 7(1): 745-758. [3]. Shahi MH, et al. BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance. PLoS One. 2015 Jun 25;10(6):e0131006. |
