2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. AT7519 Hydrochloride

AT7519 Hydrochloride 

目录号: HY-50943 纯度: 99.42%
COA 产品使用指南

摩尔计算器

AT7519 Hydrochloride 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 Hydrochloride Chemical Structure

AT7519 Hydrochloride Chemical Structure

CAS No. : 902135-91-5

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥891
In-stock
5 mg ￥810
In-stock
10 mg ￥1350
In-stock
50 mg ￥3750
In-stock
100 mg ￥5625
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of AT7519 Hydrochloride:

AT7519 Hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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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 Hydrochloride is 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)

体外研究
(In Vitro)

AT7519 Hydrochloride (0-4 μM) 在 MM 细胞中产生剂量依赖性细胞毒性，IC50 范围为 0.5 至 2 μM，并且这种诱导的细胞毒性与 GSK-3β 激活相关，与转录抑制无关。AT7519 Hydrochloride 克服了细胞因子赋予的增殖优势和 BMSC 的保护作用。AT7519 Hydrochloride (0.5 μM) 以时间依赖性方式诱导 MM 细胞凋亡。此外，AT7519 Hydrochloride (0.5 μM) 抑制 RNA 聚合酶 II CTD 的磷酸化，并部分抑制 MM.1S 细胞中的 RNA 合成[1]。AT7519 Hydrochloride (250 nM) 抑制人肿瘤细胞系的细胞周期进程。AT7519 Hydrochloride 还诱导人肿瘤细胞系的凋亡[2]。AT7519 Hydrochloride (100-700 nM) 在白血病细胞系中诱导细胞凋亡。AT7519 Hydrochloride 还抑制人类肿瘤细胞系中的转录。此外，AT7519 Hydrochloride 可抑制 RNA 聚合酶 II 并降低抗凋亡蛋白水平[3]。

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

AT7519 Hydrochloride 相关抗体:
体内研究
(In Vivo)

AT7519 Hydrochloride 在人 MM 异种移植小鼠模型中抑制肿瘤生长[1]。AT7519 Hydrochloride (4.6 和 9.1 mg/kg/剂量) 抑制早期 HCT116 肿瘤异种移植物的生长。AT7519 Hydrochloride (10 mg/kg，ip) 也抑制 HCT116 荷瘤 BALB/c 裸鼠的靶 CDKs[2]。

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

418.71

Formula

C16H18Cl3N5O2
CAS 号
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 300 mg/mL (716.49 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)

H2O 中的溶解度 : 8.33 mg/mL (19.89 mM; 超声助溶)

* "≥" 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 2.3883 mL 11.9414 mL 23.8829 mL
5 mM 0.4777 mL 2.3883 mL 4.7766 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 (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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: 99.42%

COA (273 KB) LCMS (276 KB)

产品使用指南 (1538 KB)
参考文献
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

AT7519 Hydrochloride 相关分类

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3883 mL 11.9414 mL 23.8829 mL 59.7072 mL
5 mM 0.4777 mL 2.3883 mL 4.7766 mL 11.9414 mL
10 mM 0.2388 mL 1.1941 mL 2.3883 mL 5.9707 mL
15 mM 0.1592 mL 0.7961 mL 1.5922 mL 3.9805 mL
DMSO 20 mM 0.1194 mL 0.5971 mL 1.1941 mL 2.9854 mL
25 mM 0.0955 mL 0.4777 mL 0.9553 mL 2.3883 mL
30 mM 0.0796 mL 0.3980 mL 0.7961 mL 1.9902 mL
40 mM 0.0597 mL 0.2985 mL 0.5971 mL 1.4927 mL
50 mM 0.0478 mL 0.2388 mL 0.4777 mL 1.1941 mL
60 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9951 mL
80 mM 0.0299 mL 0.1493 mL 0.2985 mL 0.7463 mL
100 mM 0.0239 mL 0.1194 mL 0.2388 mL 0.5971 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

AT7519902135-91-5AT 7519AT-7519CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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