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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 315704-66-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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
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. |
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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