PTC-209 is a novel potent and selective BMI-1 inhibitor, targeting the BMI-1 self-renewal machinery with an IC50 of ~0.5 μM. Tumor formation and, more specifically, human colorectal cancer-initiating cells (CIC) are dependent on the canonical self-renewal regulator BMI-1. Down-regulation of BMI-1 inhibits the ability of colorectal CICs to self-renew, resulting in the abrogation of their tumorigenic potential. Treatment of primary colorectal cancer xenografts with the small-molecule BMI-1 inhibitor PTC-209 resulted in colorectal CIC loss with long-term and irreversible impairment of tumor growth. Targeting the BMI-1 self-renewal machinery represents a promising approach to the elimination of many cancer stem (and initiating) cells.
CAS Number: 315704-66-6
Molecular Weight: 495.19
Chemical Name: N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PTC-209 was used at 0.5-1 µM final concentration in various in vitro assays.
PTC-209 was administered subcutaneously once a day at a dose of 60 mg/kg in primary human colon cancer xenograft models in nude mice.
- Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. (2014) Nat Med. (1):29-36.
Products are for research use only. Not for human use.
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