PI3K/HDAC-IN-1

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Data Sheet 产品使用指南技术支持

PI3K/HDAC-IN-1 是一种有效的 (PI3K/HDAC) 双重抑制剂，高效抑制 PI3Kδ 和 HDAC1 的 IC₅₀ 值分别为 8.1 nM 和 1.4 nM。

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PI3K/HDAC-IN-1 Chemical Structure

CAS No. : 2361418-52-0

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PI3K/HDAC-IN-1 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 PI3K 亚型特异性产品:

查看所有亚型

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 HDAC 亚型特异性产品:

查看所有亚型

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
纯度 & 产品资料
参考文献

生物活性

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC₅₀s of 8.1 nM and 1.4 nM, respectively^[1].

IC₅₀ & Target

PI3Kα

42 nM (IC₅₀)

PI3Kβ

101 nM (IC₅₀)

PI3Kγ

67 nM (IC₅₀)

PI3Kδ

8.1 nM (IC₅₀)

HDAC1

1.4 nM (IC₅₀)

HDAC2

3.0 nM (IC₅₀)

HDAC6

6.6 nM (IC₅₀)

HDAC8

18 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	5.2 μM Compound: 23	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 31117517]
Capan-2	IC₅₀	0.43 μM Compound: 23	Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay	[PMID: 31117517]
CHO	IC₅₀	> 30 μM Compound: 23	Inhibition of human ERG stably expressed in CHO cells by whole cell patch clamp method Inhibition of human ERG stably expressed in CHO cells by whole cell patch clamp method	[PMID: 31117517]
DU-145	IC₅₀	0.54 μM Compound: 23	Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-116	IC₅₀	0.15 μM Compound: 23	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-8	IC₅₀	0.32 μM Compound: 23	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 31117517]
HepG2	IC₅₀	1.1 μM Compound: 23	Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay	[PMID: 31117517]
HGC-27	IC₅₀	0.11 μM Compound: 23	Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay	[PMID: 31117517]
Huh-7	IC₅₀	2.5 μM Compound: 23	Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay	[PMID: 31117517]
K562	IC₅₀	6.8 μM Compound: 23	Antiproliferative activity against human K562 cells after 96 hrs by MTT assay Antiproliferative activity against human K562 cells after 96 hrs by MTT assay	[PMID: 31117517]
MCF7	IC₅₀	2 μM Compound: 23	Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-453	IC₅₀	0.3 μM Compound: 23	Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-H1299	IC₅₀	1 μM Compound: 23	Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-H460	IC₅₀	3 μM Compound: 23	Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 31117517]
Sf9	IC₅₀	> 1000 nM Compound: 23	Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	> 1000 nM Compound: 23	Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	1.4 nM Compound: 23	Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	18 nM Compound: 23	Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	3 nM Compound: 23	Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
SW1990	IC₅₀	0.9 μM Compound: 23	Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay	[PMID: 31117517]
THP-1	IC₅₀	5.4 μM Compound: 23	Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay	[PMID: 31117517]
U-87MG ATCC	IC₅₀	3.2 μM Compound: 23	Antiproliferative activity against human U87 cells after 96 hrs by MTT assay Antiproliferative activity against human U87 cells after 96 hrs by MTT assay	[PMID: 31117517]

分子量

428.46

Formula

C₂₂H₂₅FN₄O₄

CAS 号

2361418-52-0

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.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Zhang K, et al. Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J Med Chem. 2019 May 29. [Content Brief]

PI3K/HDAC-IN-1 相关分类

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3K/HDAC-IN-12361418-52-0PI3KHDACPhosphoinositide 3-kinaseHistone deacetylasesInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

PI3K/HDAC-IN-1

Customer Review

PI3K/HDAC-IN-1 相关产品

•同靶点产品:

•同靶点蛋白产品:

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参考文献

PI3K/HDAC-IN-1 相关分类

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PI3K/HDAC-IN-1

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PI3K/HDAC-IN-1 相关产品

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•同靶点蛋白产品:

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生物活性

纯度 & 产品资料

参考文献

PI3K/HDAC-IN-1 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

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