PHA-767491 (Synonyms: CAY10572)

目录号: HY-13461 纯度: 99.85%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

PHA-767491 是一种 Cdc7-Dbf4 (DDK)/Cdk9 的双重抑制剂，IC₅₀ 值分别为 10 nM 和 34 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PHA-767491 Chemical Structure

CAS No. : 845714-00-3

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
5 mg	￥500	In-stock
10 mg	￥700	In-stock
25 mg	￥1150	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Other Forms of PHA-767491:

PHA-767491 hydrochloride In-stock

MCE 顾客使用本产品发表的 3 篇科研文献

PHA-767491 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 CDK 亚型特异性产品:

查看所有亚型

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC₅₀s of 10 nM and 34 nM, respectively.

IC₅₀ & Target^[4]

CDK9

34 nM (IC₅₀)

CDK2

240 nM (IC₅₀)

CDK1

250 nM (IC₅₀)

CDK5

460 nM (IC₅₀)

GSK3-β

220 nM (IC₅₀)

Mk2

470 nM (IC₅₀)

Plk1

980 nM (IC₅₀)

Chk2

1100 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	1.07 μM Compound: 1, PHA-767491	Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
A2780	IC₅₀	1.1 μM Compound: 1	Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
A2780	IC₅₀	1.1 μM Compound: 1	Antiproliferative activity against human A2780 cells after 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs	[PMID: 18201066]
COLO 205	IC₅₀	1.5 μM Compound: 1	Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
COLO 205	IC₅₀	1.54 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human COLO205 cells after 72 hrs Antiproliferative activity against p53 deficient human COLO205 cells after 72 hrs	[PMID: 18469809]
HCT-116	IC₅₀	0.97 μM Compound: 1, PHA-767491	Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
HCT-15	IC₅₀	3.81 μM Compound: 1, PHA-767491	Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
HeLa	IC₅₀	1.83 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human HeLa cells after 72 hrs Antiproliferative activity against p53 deficient human HeLa cells after 72 hrs	[PMID: 18469809]
HT-29	IC₅₀	5 μM Compound: 1	Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
Jurkat	IC₅₀	3.2 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay	[PMID: 18469809]
K562	IC₅₀	5.87 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human K562 cells after 72 hrs Antiproliferative activity against p53 deficient human K562 cells after 72 hrs	[PMID: 18469809]
L-363	IC₅₀	1.6 μM Compound: 1	Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
MCF7	IC₅₀	1.3 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
MCF7	IC₅₀	1.33 μM Compound: 1, PHA-767491	Antiproliferative activity against human MCF7 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human MCF7 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
NCI-H929	IC₅₀	1.8 μM Compound: 1	Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
NHDF	IC₅₀	1.58 μM Compound: 1, PHA-767491	Antiproliferative activity against NHDF expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against NHDF expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
NHDF	IC₅₀	1.6 μM Compound: 1	Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay	[PMID: 19115845]
OPM-2	IC₅₀	4.5 μM Compound: 1	Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
OVCAR-8	IC₅₀	1.56 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay	[PMID: 18469809]
PC-3	IC₅₀	4.59 μM Compound: 1, PHA-767491	Antiproliferative activity against human PC3 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human PC3 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
SF-268	IC₅₀	0.86 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs	[PMID: 18469809]
SF-539	IC₅₀	2.34 μM Compound: 1, PHA-767491	Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
SW48	IC₅₀	1.2 μM Compound: 1	Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
SW480	IC₅₀	2.67 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay	[PMID: 18469809]
U2OS	IC₅₀	1.49 μM Compound: 1, PHA-767491	Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]

体外研究
(In Vitro)

PHA-767491 inhibits proliferation in both cell lines with an IC₅₀ of 0.64 µM in HCC1954 cells and 1.3 µM in Colo-205 cells. PHA-767491 is effective DDK inhibitors in vitro, with IC₅₀ values of 18.6 nM. PHA-767491 (2 µM) completely abolishes Mcm2 phosphorylation by 24 hours in HCC1954 cells^[1]. PHA-767491 in combination with 5-FU exhibits much stronger cytotoxicity and induces significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracts the 5-FU-induced phosphorylation of Chk1 and decreases the expression of the anti-apoptotic protein myeloid leukemia cell 1ine^[2]. PHA-767491 (0-10 µM) decreases glioblastoma cell viability in a time- and dose-dependent fashion, with IC₅₀ of approximately 2.5 µM for U87-MG and U251-MG cells. PHA-767491 hydrochloride induces apoptosis in glioblastoma cells, suppresses glioblastoma cell proliferation, cell migration and cell invasion^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

213.24

Formula

C₁₂H₁₁N₃O

CAS 号

845714-00-3

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (117.24 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.6896 mL	23.4478 mL	46.8955 mL
5 mM	0.9379 mL	4.6896 mL	9.3791 mL
10 mM	0.4690 mL	2.3448 mL	4.6896 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.85%

选择批次：

Data Sheet (605 KB) SDS (393 KB)

COA (284 KB) HNMR (249 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. [Content Brief]

[2]. Li W, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. Curr Cancer Drug Targets. 2015;15(3):196-204. [Content Brief]

[3]. Erbayraktar Z, et al. Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness. Cancer Cell Int. 2016 Nov 18;16:88. [Content Brief]

[4]. Montagnoli A, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. [Content Brief]

Kinase Assay ^[1]	20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 µCi (γ)-³²P ATP and 1.5 µM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl₂, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. ³²P-labeled bands are quantified using ImageJ and the IC₅₀ values are calculated using GraphPad. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC₅₀ values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. [Content Brief] [2]. Li W, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. Curr Cancer Drug Targets. 2015;15(3):196-204. [Content Brief] [3]. Erbayraktar Z, et al. Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness. Cancer Cell Int. 2016 Nov 18;16:88. [Content Brief] [4]. Montagnoli A, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. [Content Brief]

PHA-767491 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.6896 mL	23.4478 mL	46.8955 mL	117.2388 mL
	5 mM	0.9379 mL	4.6896 mL	9.3791 mL	23.4478 mL
	10 mM	0.4690 mL	2.3448 mL	4.6896 mL	11.7239 mL
	15 mM	0.3126 mL	1.5632 mL	3.1264 mL	7.8159 mL
	20 mM	0.2345 mL	1.1724 mL	2.3448 mL	5.8619 mL
	25 mM	0.1876 mL	0.9379 mL	1.8758 mL	4.6896 mL
	30 mM	0.1563 mL	0.7816 mL	1.5632 mL	3.9080 mL
	40 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9310 mL
	50 mM	0.0938 mL	0.4690 mL	0.9379 mL	2.3448 mL
	60 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9540 mL
	80 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4655 mL
	100 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL

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:

PHA-767491845714-00-3CAY10572PHA767491PHA 767491CAY 10572CAY-10572CDKCyclin dependent kinaseInhibitorinhibitorinhibit

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

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）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

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）

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

PHA-767491 (Synonyms: CAY10572)

Other Forms of PHA-767491:

PHA-767491 相关抗体

MCE 顾客使用本产品发表的 3 篇科研文献

PHA-767491 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 CDK 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

PHA-767491 相关抗体:

摩尔计算器

稀释计算器

PHA-767491 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z