AT7519 | AT7519M | CDK Inhibitor | AmBeed-信号通路专用抑制剂

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AT7519 98+%

货号：A485554 同义名： AT7519M

AT7519 is a pan-CDKs inhibitor with IC50 values of 47, 13, <10nM for CDK2/CyclinA, CDK5/p35 and CDK9/CyclinT, and modest activity against CDK1/CyclinB, CDK3/CyclinE, CDK4/CyclinD1 and CDK6/CyclinD3 with IC50 values of 210, 360, 100 and 170nM, respectively.

AT7519 化学结构
CAS号：844442-38-2

AT7519 3D分子结构
CAS号：844442-38-2

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AT7519 纯度/质量文件产品仅供科研

货号：A485554 标准纯度： 98+% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 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/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 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	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 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/CyclinE, IC50: 8 nM CDK2/CyclinA, 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/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 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	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ 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												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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。

AT7519 生物活性

靶点	CDK5 CDK5/p35, IC50:13 nM CDK4 CDK4/CyclinD1, IC50:100 nM CDK2 CDK2/CyclinA, IC50:47 nM CDK6 CDK6/CyclinD3, IC50:170 nM
描述	The CDKs (cyclin dependent kinases), as direct regulators of specific phases of the cell cycle, can control cellular proliferation and transcription with their activating cyclin partners and subunit inhibitors. Thus, the inhibition of CDKs can be assessed with monitoring the phosphorylation state of specific substrates. For example, decreased phosphorylation of the CDK1 substrate PP1 a (T320) and the CDK2 substrates Rb (T821) and NPM (T199) can indicated the inhibition of the CDKs. Decreased phosphorylation of pSer5 and pSer2 of RNA pol II CTD would indicate inhibition of CDKs 7 and 9, respectively. AT7519 is a pan-CDKs inhibitor with IC50 values of 47, 13, <10 nM for CDK2/CyclinA, CDK5/p35 and CDK9/CyclinT, and modest activity against CDK1/CyclinB, CDK3/CyclinE, CDK4/CyclinD1 and CDK6/CyclinD3 with IC50 values of 210, 360, 100 and 170 nM, respectively (measured by in vitro kinase assays)^[1]. Treatment with 0.05-1uM AT7519 for 24h was sufficient to inhibit phosphorylation of the CDK1 substrate PP1a (T320) and the CDK2 substrates Rb (T821) and NPM (T199) in HCT116 cells^[2]. AT7519 on concentration of 0.5 μM induced rapid dephosphorylation at both RNA pol II CTD at both the serine 2 and serine 5 sites^[1]. AT7519 showed antiproliferative activity and apoptosis-induction in a panel of human tumor cell lines, including ovarian carcinoma, lung carcinoma, breast carcinoma, uterine sarcoma, leukemia and lymphoma, with IC50 values ranging from 40 to 940nM. AT7519 with concentration of 250-1000nM can induce G0-G1 and G2-M cell cycle blockade in HCT116 cells. Intraperitoneal or intravenous administration of 9.1mg/kg AT7519 twice a day for 9 consecutive days achieved completely tumor regression on day 15 in HCT116 tumor xenografts^[2]. Phase 2 studies of AT7519 treatment for mantle cell lymphoma and chronic lymphocytic leukemia have been completed (see in https://www.clinicaltrials.gov/).
作用机制	The inhibition of CDK1 by AT7519 is competitive with ATP.

AT7519 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by alamar blue assay, IC50=0.35 μM	18656911
HCT116 cells		Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by Alamar blue assay, IC50=0.08 μM	26115571
MRC5 cells		Proliferation assay	72 h	Antiproliferative activity against human MRC5 cells assessed as cell viability after 72 hrs by alamar blue assay, IC50=0.98 μM	18656911

AT7519 动物研究

Dose

Mice(i.p.): min = 5 mg/kg^[2], max = 15 mg/kg^[1]

Administration

i.p.

Pharmacokinetics

Animal	Nude mice^[3]
Dose	5 mg/kg
Administration	i.v. / i.p.
C_max	1750 ng/ml (i.v.) 1886 ng/ml (i.p.)
T_1/2	1.1 h (i.v.) 1.6 h (i.p.)
AUC_0→∞	1513 h·ng/ml (i.v.) 1628 h·ng/ml (i.p.)
F	100% (i.p,)

AT7519 参考文献

[1]Santo L, Vallet S, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.

[2]Squires MS, Feltell RE, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32.

[3]Dolman ME, Poon E, et al. Cyclin-Dependent Kinase Inhibitor AT7519 as a Potential Drug for MYCN-Dependent Neuroblastoma. Clin Cancer Res. 2015 Nov 15;21(22):5100-9.

AT7519 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.08mL

2.62mL

1.31mL

26.16mL

5.23mL

2.62mL

AT7519 技术信息

CAS号	844442-38-2
分子式	C₁₆H₁₇Cl₂N₅O₂
分子量	382.245

别名	AT7519M
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(130.81 mM)，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

动物实验配方

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

AT7519 98+%

AT7519 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

AT7519 质控信息

AT7519 生物活性

AT7519 细胞研究

AT7519 动物研究

AT7519 参考文献

AT7519 实验方案

AT7519 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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CDK5	CDK5/p35, IC50:13 nM
CDK4	CDK4/CyclinD1, IC50:100 nM
CDK2	CDK2/CyclinA, IC50:47 nM
CDK6	CDK6/CyclinD3, IC50:170 nM
CDK9	CDK9/CyclinT, IC50:<10 nM
CDK3	CDK3/CyclinE, IC50:360 nM
CDK1	CDK1/CyclinB, IC50:210 nM

AT7519 98+%

AT7519 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AT7519 质控信息

AT7519 生物活性

AT7519 细胞研究

AT7519 动物研究

AT7519 参考文献

AT7519 实验方案

AT7519 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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热门区域

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AT7519 纯度/质量文件产品仅供科研