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PF-06821497
PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
Catalog No. T12430Cas No. 1844849-10-0
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Purity:97.88%
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PF-06821497
Catalog No. T12430Cas No. 1844849-10-0
PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $97 | In Stock | |
| 5 mg | $239 | In Stock | |
| 10 mg | $372 | In Stock | |
| 25 mg | $562 | In Stock | |
| 50 mg | $787 | In Stock | |
| 100 mg | $987 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $219 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition. |
| Targets&IC50 | EZH2 (Y641N):ki:<0.1 nM |
| In vitro | METHODS: U251 cells were treated with PF-06821497 (0, 50, 100 μM) and ONC201 (0, 5 μM), and cleaved PARP (clvd-PARP) and cleaved caspase 3 were analyzed by immunoblotting. RESULTS Combination treatment of PF-06821497 and ONC201 also induced more cleaved PARP in U251 cells and promoted cancer cell apoptosis. [2] |
| In vivo | METHODS: Mice bearing Karpas-422 DLBCL tumor xenografts (containing the Y641N EZH2 mutation) were treated with PF-06821497 (100,300 mg/kg, PO, twice daily) and tumor growth was observed in the mice. RESULTS Low-dose PF-06821497 can significantly inhibit tumor growth, while high-dose PF-06821497 can cause tumor regression with minimal impact on animal body weight. [1] |
| Molecular Weight | 467.34 |
| Formula | C22H24Cl2N2O5 |
| Cas No. | 1844849-10-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (117.69 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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% 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 μLddH2O 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 μLddH2O 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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