PTC-209, BMI-1 Inhibitor


Catalog No. size PriceQuantity
M60159-2D 10 mM in DMSO (0.404 mL) $131
M60159-2S 2 mg solid $133
M60159-25S 25mg solid $650

Description

Product Information
Molecular Weight: 495.19
Formula: C17H13Br2N5OS
Purity: ≥98%
CAS#: 315704-66-6
Solubility: DMSO up to 50 mM
Chemical Name: N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

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.

 


How to Use:

 

  • In vitro: PTC-209 was used at 0.5-1 µM final concentration in various in vitro assays.
  • In vivo: 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.

 

Reference:

 

  1. 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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