PF-06821497

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PF-06821497

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1844849-11-1
规格:	≥98%

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议

产品介绍

理化性质和储存条件

	Name: PF-06821497 CAS#: 1844849-11-1 Chemical Formula: C22H24Cl2N2O5 Exact Mass: 466.1062 Molecular Weight: 467.343
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Technical Information	Synonym: PF-6821497; PF6821497; PF-06821497; PF06821497; PF 6821497; PF 06821497 Chemical Name: (S)-5,8-dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one InChi Key: RXCVUHMIWHRLDF-FQEVSTJZSA-N InChi Code: 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-/m0/s1 SMILES Code: COC1=C(CN2CCC(C(Cl)=CC([C@@H](OC)C3COC3)=C4Cl)=C4C2=O)C(NC(C)=C1)=O

实验参考方法

Target	Ki:<0.1 nM (Y641N EZH2)[1].
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[1]. PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights[1]. Animal Model: Mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation)[1]. Dosage: 100 mg/kg and 300 mg/kg. Administration: PO twice daily for 31 days. Result: 100 mg/kg dose resulted in significant inhibition of tumor growth and 300 mg/kg dose minimal effected animal body weights

Target

Ki:<0.1 nM (Y641N EZH2)[1].

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[1]. PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights[1]. Animal Model: Mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation)[1]. Dosage: 100 mg/kg and 300 mg/kg. Administration: PO twice daily for 31 days. Result: 100 mg/kg dose resulted in significant inhibition of tumor growth and 300 mg/kg dose minimal effected animal body weights