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

AT7519 Hydrochloride 是一種有效的 CDK 抑制劑，對 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC50 值分別為 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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規(guī)格 價格 是否有貨 數(shù)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   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Other Forms of AT7519 Hydrochloride:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

體外研究
(In Vitro)

AT7519 Hydrochloride (0-4 μM) 在 MM 細胞中產(chǎn)生劑量依賴性細胞毒性，IC50 范圍為 0.5 至 2 μM，并且這種誘導的細胞毒性與 GSK-3β 激活相關(guān)，與轉(zhuǎn)錄抑制無關(guān)。AT7519 Hydrochloride 克服了細胞因子賦予的增殖優(yōu)勢和 BMSC 的保護作用。AT7519 Hydrochloride (0.5 μM) 以時間依賴性方式誘導 MM 細胞凋亡。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 細胞中的 RNA 合成[1]。AT7519 Hydrochloride (250 nM) 抑制人腫瘤細胞系的細胞周期進程。AT7519 Hydrochloride 還誘導人腫瘤細胞系的凋亡[2]。AT7519 Hydrochloride (100-700 nM) 在白血病細胞系中誘導細胞凋亡。AT7519 Hydrochloride 還抑制人類腫瘤細胞系中的轉(zhuǎn)錄。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.
體內(nèi)研究
(In Vivo)

AT7519 Hydrochloride 在人 MM 異種移植小鼠模型中抑制腫瘤生長[1]。AT7519 Hydrochloride (4.6 和 9.1 mg/kg/劑量) 抑制早期 HCT116 腫瘤異種移植物的生長。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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 300 mg/mL (716.49 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.42%

參考文獻
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.
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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.

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產(chǎn)品名稱：
AT7519 Hydrochloride
目錄號：
HY-50943
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