PTC-028 |
رقم الكتالوجGC37035
One-Click Copy Product Info
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PTC-028 هو مثبط متوفر بيولوجيًا عن طريق الفم لعامل الخلايا الجذعية BMI-1 في سرطان المبيضيثبط PTC-028 الخلايا السرطانية بشكل انتقائي بينما تظل الخلايا الطبيعية غير متأثرةينقص PTC-028 مؤشر كتلة الجسم 1 ، مما يؤدي إلى موت الخلايا المبرمج بوساطة كاسباس
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1782970-28-8
Sample solution is provided at 25 µL, 10mM.
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PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis[1]. BMI-1[1]
PTC-028 (25-500 nM; 48 hours) significantly decreases CP20, OVCAR4 and OV90 epithelial ovarian cancer cells viability. However, in normal ovarian surface epithelial cells (OSE) and fallopian tube epithelial cells (FTE) cells, up to 500 nM treatment with PTC-028 for 48 hours has minimal effect (~18-30% decrease)[1]. PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. PTC-028 subsequently reduces BMI-1 in the biochemical functional readout [1]. uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged [1]. PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remains unchanged compared to that of the control [1]. Significant cleavage of Caspase 7, Caspase 9 and PARP is observed in PTC-028 (100 nM; 48 hours)[1]. Cell Viability Assay[1] Cell Line: OVCAR4, OV90 and CP20 cells
PTC-028 (15 mg/kg; administered orally twice weekly) causes ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight[1].PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post dose after which plasma concentrations slowly reduce[1]. Animal Model: Female athymic nude mice with implanted OV90 cells[1]
[1]. Dey A, et al. Evaluating the Mechanism and Therapeutic Potential of PTC-028, a Novel Inhibitor of BMI-1 Function in Ovarian Cancer. Mol Cancer Ther. 2018 Jan;17(1):39-49.
| Cas No. | 1782970-28-8 | SDF | |
| Canonical SMILES | FC(C1=CC=C(NC2=NC(N3C4=CC(F)=C(F)C=C4N=C3C)=CN=C2)C=C1)(F)F | ||
| Formula | C19H12F5N5 | M.Wt | 405.32 |
| الذوبان | Soluble 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4672 mL | 12.3359 mL | 24.6719 mL |
| 5 mM | 493.4 μL | 2.4672 mL | 4.9344 mL |
| 10 mM | 246.7 μL | 1.2336 mL | 2.4672 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)