AT7519 (Synonyms: AT7519M)

目录号: HY-50940 纯度: 99.76%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

AT7519 (AT7519M) 是一种有效的 CDK 抑制剂，对 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC₅₀ 值分别为 210，47，100，13，170 和 <10 nM。

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AT7519 Chemical Structure

CAS No. : 844442-38-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥891	In-stock
5 mg	￥810	In-stock
10 mg	￥1350	In-stock
50 mg	￥4450	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

Other Forms of AT7519:

AT7519 TFA In-stock
AT7519 Hydrochloride In-stock

MCE 顾客使用本产品发表的 12 篇科研文献

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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

AT7519 (AT7519M) as a potent inhibitor of CDKs, with IC₅₀s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

IC₅₀ & Target^[2]

CDK9/Cyclin T

10 nM (IC₅₀)

CDK5/p35

13 nM (IC₅₀)

cdk2/cyclin A

47 nM (IC₅₀)

Cdk4/cyclin D1

100 nM (IC₅₀)

cdk6/cyclin D3

170 nM (IC₅₀)

Cdk1/cyclin B

210 nM (IC₅₀)

CDK7/Cyclin H/MAT1

2400 nM (IC₅₀)

GSK3β

89 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2058	IC₅₀	0.166 μM Compound: AT7519	Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay	[PMID: 33611192]
A2780	IC₅₀	350 nM Compound: 33	Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by alamar blue assay Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by alamar blue assay	[PMID: 18656911]
ASPC1	IC₅₀	533 nM Compound: AT7519	Antiproliferative activity against human AsPC1 cells after 72 hrs by prestoblue assay Antiproliferative activity against human AsPC1 cells after 72 hrs by prestoblue assay	[PMID: 30343954]
BXPC-3	IC₅₀	640 nM Compound: AT7519	Antiproliferative activity against human BxPC3 cells after 72 hrs by prestoblue assay Antiproliferative activity against human BxPC3 cells after 72 hrs by prestoblue assay	[PMID: 30343954]
HCT-116	IC₅₀	0.082 μM Compound: 33	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by alamar blue assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by alamar blue assay	[PMID: 18656911]
HCT-116	IC₅₀	132 nM Compound: AT7519	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by cell titer glo-based luminescence assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by cell titer glo-based luminescence assay	[PMID: 31175010]
HCT-116	IC₅₀	80 nM Compound: AT7519	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by Alamar blue assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by Alamar blue assay	[PMID: 26115571]
MIA PaCa-2	IC₅₀	411 nM Compound: AT7519	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by prestoblue assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by prestoblue assay	[PMID: 30343954]
MRC5	IC₅₀	> 10000 nM Compound: 33	Antiproliferative activity against human MRC5 nonprolifreative cells assessed as cell viability after 72 hrs by alamar blue assay Antiproliferative activity against human MRC5 nonprolifreative cells assessed as cell viability after 72 hrs by alamar blue assay	[PMID: 18656911]
MRC5	IC₅₀	0.425 μM Compound: AT7519	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay	[PMID: 33611192]
MRC5	IC₅₀	980 nM Compound: 33	Antiproliferative activity against human MRC5 cells assessed as cell viability after 72 hrs by alamar blue assay Antiproliferative activity against human MRC5 cells assessed as cell viability after 72 hrs by alamar blue assay	[PMID: 18656911]
MV4-11	IC₅₀	0.391 μM Compound: AT7519	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay	[PMID: 33611192]
PC-3	IC₅₀	0.71 μM Compound: 1; AT-7519	Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 31846828]
Sf21	IC₅₀	< 10 nM Compound: AT7519	Inhibition of recombinant human full-length C-terminal His6-tagged CDK9/human full-length untagged cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate Inhibition of recombinant human full-length C-terminal His6-tagged CDK9/human full-length untagged cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate	[PMID: 30543440]
Sf21	IC₅₀	210 nM Compound: AT7519	Inhibition of recombinant full-length human C-terminal His6-tagged CDK1/human full-length N-terminal GST-tagged Cyclin B expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate measured after 2 hrs in presence of gamma[32P] ATP b Inhibition of recombinant full-length human C-terminal His6-tagged CDK1/human full-length N-terminal GST-tagged Cyclin B expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate measured after 2 hrs in presence of gamma[32P] ATP b	[PMID: 30543440]
Sf21	IC₅₀	2400 nM Compound: AT7519	Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs	[PMID: 30543440]
Sf21	IC₅₀	360 nM Compound: AT7519	Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate	[PMID: 30543440]

体外研究
(In Vitro)

AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC₅₀s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells^[1]. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines^[2]. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels^[3].

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

体内研究
(In Vivo)

AT7519 inhibits tumor growth in a human MM xenograft mouse model^[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice^[2].

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

Clinical Trial

分子量

382.24

Formula

C₁₆H₁₇Cl₂N₅O₂

CAS 号

844442-38-2

性状

固体

颜色

White to off-white

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (130.81 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6161 mL	13.0806 mL	26.1613 mL
5 mM	0.5232 mL	2.6161 mL	5.2323 mL
10 mM	0.2616 mL	1.3081 mL	2.6161 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.54 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.54 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.54 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.76%

选择批次：

Data Sheet (632 KB) SDS (393 KB)

COA (196 KB) HNMR (270 KB) LCMS (107 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Santo L, 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. [Content Brief]

[2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. [Content Brief]

[3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8. [Content Brief]

Cell Assay ^[1]	AT7519's effects on viability of MM cell lines, primary MM cells, and PBMNCs is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). MM cells (2-3 × 10⁴ cells/well) are incubated in 96-well culture plates with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation is measured. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	To evaluate the in vivo anti-MM activity of AT7519, male SCID mice are inoculated subcutaneously with 5×10⁶ MM.1S cells in 100 μL serum-free RPMI 1640 medium. When tumors are measurable, mice are treated intraperitoneally (IP) with vehicle or AT7519 dissolved in saline 0.9%. The first group of 10 mice is treated with 15 mg/kg once a day for five days for 2 weeks, and the second group is treated with 15 mg/kg once a day three times a week for four consecutive weeks. The control group receives the carrier alone at the same schedule. Tumor size is measured every alternate day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V= 0.5 a × b² (a= long diameter of the tumor, b= short diameter of the tumor). Animals are sacrificed when the tumor reaches 2 cm³ or when the tumor is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Santo L, 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. [Content Brief] [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. [Content Brief] [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8. [Content Brief]

AT7519 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	2.6161 mL	13.0806 mL	26.1613 mL	65.4032 mL
	5 mM	0.5232 mL	2.6161 mL	5.2323 mL	13.0806 mL
	10 mM	0.2616 mL	1.3081 mL	2.6161 mL	6.5403 mL
	15 mM	0.1744 mL	0.8720 mL	1.7441 mL	4.3602 mL
	20 mM	0.1308 mL	0.6540 mL	1.3081 mL	3.2702 mL
	25 mM	0.1046 mL	0.5232 mL	1.0465 mL	2.6161 mL
	30 mM	0.0872 mL	0.4360 mL	0.8720 mL	2.1801 mL
	40 mM	0.0654 mL	0.3270 mL	0.6540 mL	1.6351 mL
	50 mM	0.0523 mL	0.2616 mL	0.5232 mL	1.3081 mL
	60 mM	0.0436 mL	0.2180 mL	0.4360 mL	1.0901 mL
	80 mM	0.0327 mL	0.1635 mL	0.3270 mL	0.8175 mL
	100 mM	0.0262 mL	0.1308 mL	0.2616 mL	0.6540 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:

AT7519844442-38-2AT7519MAT 7519AT-7519CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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AT7519 (Synonyms: AT7519M)

Customer Review

Other Forms of AT7519:

MCE 顾客使用本产品发表的 12 篇科研文献

AT7519 相关产品

•相关化合物库:

•同靶点产品:

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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

摩尔计算器

稀释计算器

AT7519 相关分类

完整储备液配制表

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AT7519 (Synonyms: AT7519M)

Customer Review

Other Forms of AT7519:

AT7519 相关抗体

MCE 顾客使用本产品发表的 12 篇科研文献

AT7519 相关产品

•相关化合物库:

•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

AT7519 相关抗体:

摩尔计算器

稀释计算器

AT7519 相关分类

完整储备液配制表

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