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PTC-209 Bmi-1 inhibitor,cell-permeable and small-molecule

Catalog No.B3179
Size Price Stock Qty
10mM (in 1mL DMSO)
$280.00
In stock
2mg
$89.00
In stock
5mg
$100.00
In stock
10mg
$160.00
In stock
50mg
$470.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

PTC-209

Biological Activity

Description PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 µM.
Targets BMI-1          
IC50 0.5 µM          

Protocol

Cell experiment [1]:

Cell lines

Human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

37oC

Applications

PTC-209 dose-dependently inhibits not only the UTR-mediated reporter expression but also endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells (IC50 = ~0.5 μM). PTC-209 (between 0.1 and 10 μM) also reduces BMI-1 protein levels in a dose-dependent manner with a concomitant reduction in cell growth.

Animal experiment [1]:

Animal models

Primary human colon cancer xenograft in nude mice

Dosage form

Administered subcutaneously once a day at a dose of 60 mg per kg body weight

Applications

For mice transplanted with cells from sample 01, 9 d following the initial drug administration, the tumor volume of the PTC-209–treated group is significantly reduced, continued treatment of animals with PTC-209 for an additional week did not affect the overall health of the mice, and tumors did not increase in size. Likewise, for mice given cells from sample 03, 9 d after PTC-209 initiation, the drug-treated tumors displays a significantly smaller tumor volume as compared to the control tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Kreso A, van Galen P, Pedley NM et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

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Chemical Properties

Cas No. 315704-66-6 SDF Download SDF
Chemical Name N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-1,3-thiazol-2-amine
Canonical SMILES CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br
Formula C17H13Br2N5OS M.Wt 495.19
Solubility >24.8mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 µM [1].

PTC-209 is screened out by using gene expression modulation by small molecules (GEMS) technology. It can lower BMI-1 transcript levels. PTC-209 is demonstrated to inhibit not only the UTR-mediated expression but also endogenous BMI-1 expression in HCT116 cell line. For HEK293 and HT1080 cell lines, PTC-209 doesn’t show any inhibition of the growth, suggesting that PTC-209 has no cytotoxicity. And for tumor cells or stem cells, such as U937, HT1080 and human hematopoietic stem cells, PTC-209 can inhibit the proliferation of them. As BMI-1 plays its role through the PRC1 complex, PTC-209 reduces the ability of PRC1 selectively. It is also reported that PTC-209 suppresses the growth of colorectal tumor cells through irreversible growth inhibition of CICs [1].

References:
[1] Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L, Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN, Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.