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PF-06821497

🥰Excellent
Catalog No. T12430Cas No. 1844849-10-0
Alias Mevrometostat

PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.

PF-06821497

PF-06821497

🥰Excellent
Purity: 97.88%
Catalog No. T12430Alias MevrometostatCas No. 1844849-10-0
PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
Pack SizePriceAvailabilityQuantity
1 mg$97In Stock
5 mg$239In Stock
10 mg$372In Stock
25 mg$562In Stock
50 mg$787In Stock
100 mg$987In Stock
1 mL x 10 mM (in DMSO)$219In Stock
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Purity:97.88%
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Product Introduction

Bioactivity
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]
AliasMevrometostat
Chemical Properties
Molecular Weight467.34
FormulaC22H24Cl2N2O5
Cas No.1844849-10-0
SmilesClC1=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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.1398 mL10.6988 mL21.3977 mL106.9885 mL
5 mM0.4280 mL2.1398 mL4.2795 mL21.3977 mL
10 mM0.2140 mL1.0699 mL2.1398 mL10.6988 mL
20 mM0.1070 mL0.5349 mL1.0699 mL5.3494 mL
50 mM0.0428 mL0.2140 mL0.4280 mL2.1398 mL
100 mM0.0214 mL0.1070 mL0.2140 mL1.0699 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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