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Purity: ≥98%
PF-06726304 is a novel, potent and selective SAM-competitive EZH2 (enhancer of zeste homolog 2) inhibitor with a Ki of 0.7 nM. PF-06726304 displayed improved LipE and on-target potency in both biochemical and cellular readouts relative to compound 18. PF-06726304 also displayed robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.
| ln Vitro |
PF-06726304 (Compound 31) inhibits Karpas-422 H3K27me3 with an IC50 of 15 nM [1]. PF-06726304, with an IC50 of 25 nM, suppresses the growth of Karpas-422 cells carrying wild-type EZH2[1].
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| ln Vivo |
In a subcutaneous Karpas-422 xenograft model, PF-06726304 (200 and 300 mg/kg; BID 20 days) suppresses tumor development and causes a strong modification of downstream indicators [1].
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| Animal Protocol |
Animal/Disease Models: Female Scid beige mice (6-8 weeks old) using Karpas-422 xenograft model [1]
Doses: 200 and 300 mg/kg Route of Administration: BID for 20 days Experimental Results: Inhibited tumor growth and induced downstream organisms Robust modulation of markers in a subcutaneousKarpas-422 xenograft model. |
| References |
[1]. Kung PP, et al. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. J Med Chem. 2016 Sep 22;59(18):8306-25.
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| Molecular Formula |
C22H21CL2N3O3
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|---|---|
| Molecular Weight |
446.326443433762
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| CAS # |
1616287-82-1
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| Related CAS # |
PF-06726304 acetate;2080306-28-9
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| SMILES |
O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl
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| InChi Key |
PDKDOPJQPKXNCT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21Cl2N3O3/c1-10-7-11(2)25-21(28)16(10)9-27-6-5-14-17(23)8-15(20(24)19(14)22(27)29)18-12(3)26-30-13(18)4/h7-8H,5-6,9H2,1-4H3,(H,25,28)
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| Chemical Name |
5,8-Dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone
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| Synonyms |
PF-6726304; PF 6726304; PF6726304; PF-06726304; PF 06726304; PF06726304;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 15 mg/mL (~33.61 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2405 mL | 11.2025 mL | 22.4049 mL | |
| 5 mM | 0.4481 mL | 2.2405 mL | 4.4810 mL | |
| 10 mM | 0.2240 mL | 1.1202 mL | 2.2405 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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