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PARP/EZH2-IN-2
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Catalog No. T208807
PARP/EZH2-IN-2 (compound 12e) functions as a dual inhibitor targeting both PARP1 and EZH2, with IC50 values of 6.89 and 27.34 nM, respectively. This compound exhibits anticancer activity without toxicity to normal cells, achieving synthetic lethality indirectly by increasing PARP1 sensitivity through EZH2 inhibition, and inducing cell death by modulating excessive autophagy.
PARP/EZH2-IN-2
PARP/EZH2-IN-2
😃Good
Catalog No. T208807
PARP/EZH2-IN-2 (compound 12e) functions as a dual inhibitor targeting both PARP1 and EZH2, with IC50 values of 6.89 and 27.34 nM, respectively. This compound exhibits anticancer activity without toxicity to normal cells, achieving synthetic lethality indirectly by increasing PARP1 sensitivity through EZH2 inhibition, and inducing cell death by modulating excessive autophagy.
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| 50 mg | Inquiry | Backorder | Backorder |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
| Description | PARP/EZH2-IN-2 (compound 12e) functions as a dual inhibitor targeting both PARP1 and EZH2, with IC50 values of 6.89 and 27.34 nM, respectively. This compound exhibits anticancer activity without toxicity to normal cells, achieving synthetic lethality indirectly by increasing PARP1 sensitivity through EZH2 inhibition, and inducing cell death by modulating excessive autophagy. |
| Targets&IC50 | EZH2:27.34 ± 1 nM, PARP1:6.89 ± 0.7 nM |
| In vitro | PARP/EZH2-IN-2 (compound 12e) exhibits optimal cytotoxicity with IC50 values of 2.84 μM against MDA-MB-231 cells and 0.91 μM against BT-549 cells, while showing no toxicity to normal breast cell lines. |
| In vivo | PARP/EZH2-IN-2 (compound 12e) demonstrates superior antitumor activity compared to Niraparib combined with GSK126 when administered via intraperitoneal injection at doses of 20-50 mg/kg. |
| Formula | C33H31N7O3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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