PF-06726304

EZH1/2 抑制剂

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货号 (SKU)	包装规格	是否现货
P414027-2mg	2mg	期货
P414027-5mg	5mg	期货
P414027-10mg	10mg	现货
P414027-25mg	25mg	期货
P414027-50mg	50mg	现货

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基本描述

英文别名	PF-67263041(2H)-Isoquinolinone,5,8-dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-
规格或纯度	≥99%
英文名称	PF-06726304
生化机理	PF-06726304 是一种选择性 EZH2 抑制剂，对 WT EZH2 和 Y641N 的 Ki 值分别为 0.7 nM 和 3 nM；还能抑制 H3K27me3，IC50 值为 15 nM。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM. Targets Ezh2 (wild-type) (cell-free); EZH2 Y641N (cell-free) 0.7 nM(Ki); 3 nM(Ki) In vitro PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction and antiproliferation effect. In vivo PF-06726304 displays robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes. PF-06726304 displays good efficacy in a diffuse large B-cell lymphoma Karpas-422 tumor model and exhibited on-target pharmacodynamic effects in vivo. Cell Research(from reference) Cell lines：Karpas-422 cell line Incubation Time：72 h
纯度	≥99%

EZH2 Tclin 组蛋白赖氨酸N-甲基转移酶EZH2(Histone-lysine N-methyltransferase EZH2) (8 活性数据)

点击查看靶蛋白信息： EZH2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

Liver (3974 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (2012 活性数据)

点击查看靶蛋白信息： EZH2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

PubChem SID	504772508
分子类型	小分子
IIUPAC Name	5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1-one
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)
InChi Key	PDKDOPJQPKXNCT-UHFFFAOYSA-N
Smiles	CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C4=C(ON=C4C)C)Cl)C
Isomeric SMILES	CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C4=C(ON=C4C)C)Cl)C
PubChem CID	86723730
分子量	446.33

溶解性	Solubility (25°C) In vitro Ethanol: 22 mg/mL (49.29 mM); DMSO: 10 mg/mL (22.4 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	10
DMSO(mM) Max Solubility	22.40494701
Water(mg / mL) Max Solubility	＜1
分子量	446.300 g/mol
XLogP3	3.600
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	4
可旋转键计数Rotatable Bond Count	3
精确质量Exact Mass	445.096 Da
单同位素质量Monoisotopic Mass	445.096 Da
拓扑极表面积Topological Polar Surface Area	75.400 Å²
重原子数Heavy Atom Count	30
形式电荷Formal Charge	0
复杂度Complexity	798.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1