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PI3K/HDAC-IN-2
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。
PI3K/HDAC-IN-2图片
CAS NO:2361418-65-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PI3K/HDAC-IN-2 是一种有效的双重PI3K/HDAC抑制剂,对 PI3Kα、PI3Kβ、PI3Kγ、PI3Kδ的IC50分别为 226 nM、279 nM、467 nM、29 nM,对于 HDAC1、HDAC2、HDC4、HDAC6、HDAC8,IC50分别为 1.3 nM、3.4 nM、972 nM、17 nM、12 nM。PI3K/HDAC-IN-2 表现出 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性。PI3K/HDAC-IN-2具有显着的抗癌作用。
生物活性

PI3K/HDAC-IN-2 is a potent dualPI3K/HDACinhibitor withIC50s of 226 nM, 279 nM, 467 nM, 29 nM forPI3Kα,PI3Kβ,PI3Kγ,PI3Kδ, respectively, andIC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM forHDAC1,HDAC2, HDC4,HDAC6,HDAC8, respectively. PI3K/HDAC-IN-2 exhibitsPI3Kδand class I and IIbHDACselectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].

IC50& Target[1]

PI3Kα

226 nM (IC50)

PI3Kβ

279 nM (IC50)

PI3Kγ

467 nM (IC50)

PI3Kδ

29 nM (IC50)

HDAC1

1.3 nM (IC50)

HDAC2

3.4 nM (IC50)

HDAC4

972 nM (IC50)

HDAC6

17 nM (IC50)

HDAC8

12 nM (IC50)

体外研究
(In Vitro)

For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively[1].
PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM[1].

体内研究
(In Vivo)

In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM[1].

分子量

461.47

Formula

C23H23N7O4

CAS 号

2361418-65-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.