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PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
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 |
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] |
Alias | Mevrometostat |
Molecular Weight | 467.34 |
Formula | C22H24Cl2N2O5 |
Cas No. | 1844849-10-0 |
Smiles | ClC1=C2C(=C(Cl)C=C1[C@H](OC)C3COC3)CCN(CC4=C(OC)C=C(C)NC4=O)C2=O |
Relative Density. | 1.41 g/cm3 (Predicted) |
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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