PHA-767491 hydrochloride | CDK | AmBeed-信号通路专用抑制剂

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PHA-767491 hydrochloride {[allProObj[0].p_purity_real_show]}

货号：A669599

PHA-767491 hydrochloride是一种 ATP 竞争性 Cdc7/Cdk9 抑制剂，IC50 分别为 10 nM 和 34 nM，选择性显著高于其他相关激酶，用于细胞周期研究。

PHA-767491 hydrochloride 化学结构
CAS号：942425-68-5

PHA-767491 hydrochloride 3D分子结构
CAS号：942425-68-5

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PHA-767491 hydrochloride 纯度/质量文件产品仅供科研

货号：A669599 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

PHA-767491 hydrochloride 生物活性

靶点	CDK5 CDK5, IC50:460 nM CDK2 CDK2, IC50:240 nM CDK9 CDK9, IC50:34 nM Cdc Cdc7, IC50:10 nM CDK1 CDK1, IC50:250 nM
描述	Cdc7 is an essential kinase that promotes DNA replication by activating origins of replication. PHA-767491 is an effective, ATP-competitive, dual Cdc7/CDK9 inhibitor with IC₅₀s of 10 nM and 34 nM, respectively. Cell proliferation was inhibited in a panel of 61 human cell lines challenged with low micromolar concentrations of PHA-767491, with an average IC₅₀ value of 3.17 mM and less than 10 mM in all cases. In a smaller panel of 17 different cell types, using sub-G1 DNA content as a parameter of apoptosis, 24 h of exposure to either 5 or 10 mM PHA-767491 was sufficient to cause cell death. Importantly, PHA-767491 is capable of preventing duplication, and it can kill both p53-positive and p53-negative tumor cells of different origins. Treatment with 5 mM PHA-767491 for 6 to 9 hours in HeLa cells was necessary to observe a marked decrease in the number of bromodeoxyuridine (BrdU)-positive cells. After intravenous administration at two dose levels of 20 and 30 mg/kg twice a day for five consecutive days in nude mice carrying subcutaneous implanted tumors, a dose-dependent reduction in tumor volume with respect to vehicle-treated animals was observed^[3].
作用机制	PHA-767491 competes with ATP for binding site, thus behaving as a pure ATP competitor.

PHA-767491 hydrochloride 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=1.07 μM	18469809
human COLO205 cells		Proliferation assay	72 h	Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay, IC50=1.5 μM	19115845
human HCT116 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=0.97 μM	18469809
human HCT15 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=3.81 μM	18469809

PHA-767491 hydrochloride 动物研究

Dose	Mice: 20 mg/kg, 30 mg/kg^[3] (i.v., BID); 25 mg/kg^[4] (i.p.)
Administration	i.v., i.p.

PHA-767491 hydrochloride 参考文献

[1]Natoni A, Murillo LS, et al. Mechanisms of action of a dual Cdc7/Cdk9 kinase inhibitor against quiescent and proliferating CLL cells. Mol Cancer Ther. 2011 Sep;10(9):1624-34.

[2]Swords R, Mahalingam D, et al. Cdc7 kinase - a new target for drug development. Eur J Cancer. 2010 Jan;46(1):33-40.

[3]Montagnoli A, Valsasina B, Croci V, Menichincheri M, Rainoldi S, Marchesi V, Tibolla M, Tenca P, Brotherton D, Albanese C, Patton V, Alzani R, Ciavolella A, Sola F, Molinari A, Volpi D, Avanzi N, Fiorentini F, Cattoni M, Healy S, Ballinari D, Pesenti E, Isacchi A, Moll J, Bensimon A, Vanotti E, Santocanale C. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. doi: 10.1038/nchembio.90. Epub 2008 May 11. PMID: 18469809.

PHA-767491 hydrochloride 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.00mL

0.80mL

0.40mL

20.02mL

4.00mL

2.00mL

40.05mL

8.01mL

4.00mL

PHA-767491 hydrochloride 技术信息

CAS号	942425-68-5
分子式	C₁₂H₁₂ClN₃O
分子量	249.696

别名
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

溶解度

DMSO: 16 mg/mL(64.08 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 50 mg/mL(200.24 mM)，配合低频超声助溶

动物实验配方

5% DMSO+30% PEG 300+2% Tween 80+water 1 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=1.07 μM	18469809
human COLO205 cells		Proliferation assay	72 h	Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay, IC50=1.5 μM	19115845
human HCT116 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=0.97 μM	18469809
human HCT15 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=3.81 μM	18469809
human HCT16 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT16 cells after 72 hrs by luciferase based assay, IC50=1 μM	19115845
human HeLa cells	5 μM	Function assay	24 h	Induction of apoptosis in human HeLa cells assessed as appearance of PARP at 5 uM after 24 hrs	18469809
human HT-29 cells		Proliferation assay	72 h	Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay, IC50=5 μM	19115845
human Jurkat cells		Proliferation assay	72 h	Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay, IC50=3.2 μM	18469809
human K562 cells		Proliferation assay	72 h	Antiproliferative activity against p53 deficient human K562 cells after 72 hrs, IC50=5.87 μM	18469809
human L363 cells		Proliferation assay	72 h	Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay, IC50=1.6 μM	19115845
human MCF7 cells		Proliferation assay	72 h	Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay, IC50=1.3 μM	19115845
human NCI60 cells		Proliferation assay		Antiproliferative activity against human NCI60 cells, IC50=3.1 μM	18469809
human NCI-H929 cells		Proliferation assay	72 h	Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay, IC50=1.8 μM	19115845
human NHDF cells		Proliferation assay	72 h	Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay, IC50=1.6 μM	19115845
human OPM2 cells		Proliferation assay	72 h	Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay, IC50=4.5 μM	19115845
human OVCAR8 cells		Proliferation assay	72 h	Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay, IC50=1.56 μM	18469809
human SF268 cells		Proliferation assay	72 h	Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs, IC50=0.86 μM	18469809
human SF539 cells		Proliferation assay	72 h	Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=2.34 μM	18469809
human SW403 cells		Proliferation assay	72 h	Antiproliferative activity against human SW403 cells after 72 hrs by luciferase based assay, IC50=1 μM	19115845
human SW48 cells		Proliferation assay	72 h	Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay, IC50=1.2 μM	19115845
human SW480 cells		Proliferation assay	72 h	Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay, IC50=2.67 μM	18469809
human U2OS cells		Proliferation assay	72 h	Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay, IC50=1.49 μM	18469809
NHDF	5 μM	Function assay	16 h	Induction of cell cycle arrest in thymidine deficient NHDF assessed as DNA synthesis in S-phase at 5 uM after 16hrs FACS analysis in presence of serum	18469809
U937 cells		Function assay		Inhibition of TNFalpha production in U937 cells, IC50=19 μM	17480064

PHA-767491 hydrochloride {[allProObj[0].p_purity_real_show]}

PHA-767491 hydrochloride 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PHA-767491 hydrochloride 质控信息

PHA-767491 hydrochloride 生物活性

PHA-767491 hydrochloride 细胞研究

PHA-767491 hydrochloride 动物研究

PHA-767491 hydrochloride 参考文献

PHA-767491 hydrochloride 实验方案

PHA-767491 hydrochloride 技术信息

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CDK5	CDK5, IC50:460 nM
CDK2	CDK2, IC50:240 nM
CDK9	CDK9, IC50:34 nM
Cdc	Cdc7, IC50:10 nM
CDK1	CDK1, IC50:250 nM

PHA-767491 hydrochloride {[allProObj[0].p_purity_real_show]}

PHA-767491 hydrochloride 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PHA-767491 hydrochloride 质控信息

PHA-767491 hydrochloride 生物活性

PHA-767491 hydrochloride 细胞研究

PHA-767491 hydrochloride 动物研究

PHA-767491 hydrochloride 参考文献

PHA-767491 hydrochloride 实验方案

PHA-767491 hydrochloride 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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PHA-767491 hydrochloride 纯度/质量文件产品仅供科研