PF-06821497


Catalog No. Size PriceQuantity
M25655-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.

Product information

CAS Number: 1844849-10-0

Molecular Weight: 467.34

Formula: C22H24Cl2N2O5

Chemical Name: 5,8-dichloro-7-[(R)-methoxy(oxetan-3-yl)methyl]-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-1,2,3,4-tetrahydroisoquinolin-1-one

Smiles: CC1=CC(OC)=C(CN2CCC3=C(Cl)C=C([C@H](OC)C4COC4)C(Cl)=C3C2=O)C(=O)N1

InChiKey: RXCVUHMIWHRLDF-HXUWFJFHSA-N

InChi: InChI=1S/C22H24Cl2N2O5/c1-11-6-17(29-2)15(21(27)25-11)8-26-5-4-13-16(23)7-14(19(24)18(13)22(26)28)20(30-3)12-9-31-10-12/h6-7,12,20H,4-5,8-10H2,1-3H3,(H,25,27)/t20-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

PF-06821497 (compound 23a: 100 mg/kg, PO twice daily for 31 days) treatment results in significant inhibition of tumor growth, and the the tumor regressition effect can be sustained for another 40 days after the terminal administration. PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights.

Products are for research use only. Not for human use.

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