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PTC-209

Katalog-Nr.GC15725

PTC-209, eine niedermolekulare Verbindung, die selektiv BMI-1 hemmt mit einer IC50 von 0,5 µM in HT1080-Zellen, ist ein vielversprechendes Antikrebsmittel.

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PTC-209 Chemische Struktur

Cas No.: 315704-66-6

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10mM (in 1mL DMSO)
190,00 $
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2mg
65,00 $
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5mg
73,00 $
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10mg
117,00 $
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50mg
324,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

various cancer cell lines: lung (LNM35, A549), breast (MDA-MB-231 and T47D), and colon (HT-29, HCT-116, and HCT8/S11)

Preparation Method

Cells were seeded at a density of 5000 cells/well into 96-well plates. After 24h, cells were treated for another 24, 48, and 72h with increasing concentrations of PTC-209 (0.01-10 µM) in triplicate. Control cultures were treated with 0.1% DMSO (the drug vehicle).

Reaction Conditions

0.01-10µM PTC-209 for 24, 48, and 72h

Applications

PTC-209 induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested. Lung cancer cells (LNM35 and A549) showed a higher sensitivity to PTC-209 treatment compared with breast (MDA-MB-231) and colon (HT-29) cancer cells.

Animal experiment [2]:

Animal models

female nude mice, four to six weeks old

Preparation Method

MDA-MB-231 cells were exposed to PTC-209, palbociclib, or combination of the two inhibitors at 5.0µM for 72h. Cells were then trypsinized, washed with PBS, and 2×106 cells were subcutaneously injected into the right left frank of female nude mice in a 100µL mixture (1:1 v/v of PBS/matrigel). The animals were monitored twice weekly and tumor volume was measured using caliper.

Dosage form

MDA-MB-231 cells were exposed to drugs at 5.0µM for 72h

Applications

PTC-209 and palbociclib significantly inhibit the growth of tumor, and combination of both drugs was more efficacious in inhibiting MDA-MB-231 tumor growth in vivo. PTC-209 and palbociclib treatments restricted the invasiveness of MDA-MB-231 cells, while combination group exhibited the most profound restricted invasion of tumor cells compared to other treatment groups and control.

References:

[1]. Sulaiman S, Arafat K, et al. PTC-209 Anti-Cancer Effects Involved the Inhibition of STAT3 Phosphorylation. Front Pharmacol. 2019;10:1199. Published 2019 Oct 21.

[2]. Elango R, Vishnubalaji R, et al. Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo. Sci Rep. 2019;9(1):13696. Published 2019 Sep 23.

Background

PTC-209, eine niedermolekulare Verbindung, die selektiv BMI-1 mit einer IC50 von 0,5 µM in HT1080-Zellen hemmt, ist ein vielversprechendes Antikrebsmittel.

In vitro reduziert PTC-209 in menschlichen Darmkrebszellen bei Dosierungen zwischen 0,1 und 10 µM die BMI-1-Proteinwerte dosisabhängig und führt zu einer gleichzeitigen Reduktion des Zellwachstums. PTC-209 verursacht eine konzentrations- und zeitabhängige Abnahme der zellulären Vitalität von Lungenkrebszellen (LNM35 und A549), Brustkrebszellen (MDA-MB-231 und T47D) sowie Darmkrebszellen (HT-29, HCT8/S11 und HCT-116). Die Behandlung mit PTC-209 verringerte signifikant die Anzahl lebensfähiger Zellen in humanen Multiplen Myelomzelllinien, induzierte einen G1-Zellzyklusarrest, förderte Apoptose und zeigte synergistische Aktivität mit Pomalidomid und Carfilzomib. Im MM-Mikroumgebung beeinträchtigte PTC-209 die Röhrenbildung, hemmte die Entwicklung von Osteoklasten sowie die Bildung von Osteoblasten dosisabhängig (P < 0,01 bei 1 μM). Die therapeutische Zielsetzung von BMI-1 durch PTC-209 ist ein vielversprechender neuartiger therapeutischer Eingriff für das MM.

PTC-209 in Kombination mit Palbociclib hemmt die Proliferation von Tumorzellen, die Bildung von Sphären und Kolonien, Migration und in vivo Tumorwachstum[4]. Die Verabreichung von PTC-209 reduzierte signifikant das Tumorwachstum in einem HNSCC-Xenograftmodell durch Bmi1-Hemmung und beeinträchtigte die Zellproliferation in vivo[5]. PTC-209 schwächt das Wachstum von Glioblastomen signifikant ab, wie ein murines orthotopes Xenograftmodell zeigt[6].

References:
[1].Kreso A, van Galen P, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014;20(1):29-36.
[2].Sulaiman S, Arafat K, et al. PTC-209 Anti-Cancer Effects Involved the Inhibition of STAT3 Phosphorylation. Front Pharmacol. 2019;10:1199. Published 2019 Oct 21.
[3].Bolomsky A, Schlangen K, et al. Targeting of BMI-1 with PTC-209 shows potent anti-myeloma activity and impairs the tumour microenvironment. J Hematol Oncol. 2016;9:17. Published 2016 Mar 2.
[4]. Elango R, Vishnubalaji R, et al. Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo. Sci Rep. 2019;9(1):13696. Published 2019 Sep 23.
[5].Wang Q, Li Z, et al. Pharmacological inhibition of Bmi1 by PTC-209 impaired tumor growth in head neck squamous cell carcinoma. Cancer Cell Int. 2017;17:107. Published 2017 Nov 21.
[6].Kong Y, Ai C, et al. Targeting of BMI-1 with PTC-209 inhibits glioblastoma development. Cell Cycle. 2018;17(10):1199-1211

Chemical Properties

Cas No. 315704-66-6 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
Löslichkeit ≥ 24.75mg/mL in DMSO Storage Store at -20° C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0194 mL 10.0971 mL 20.1943 mL
5 mM 0.4039 mL 2.0194 mL 4.0389 mL
10 mM 0.2019 mL 1.0097 mL 2.0194 mL
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