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

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.

Product information

CAS Number: 315704-66-6

Molecular Weight: 495.19

Formula: C17H13Br2N5OS

Chemical Name: N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine

Smiles: CC1N=C2N=CC=CN2C=1C1=CSC(NC2C(Br)=CC(=CC=2Br)OC)=N1

InChiKey: XVOOCQSWCCRVDY-UHFFFAOYSA-N

InChi: InChI=1S/C17H13Br2N5OS/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)

Technical Data

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

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.

References:

  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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