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

AT7519 (AT7519M) 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 Chemical Structure

AT7519 Chemical Structure

CAS No. : 844442-38-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥891
In-stock
5 mg ￥810
In-stock
10 mg ￥1350
In-stock
50 mg ￥4450
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100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of AT7519:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)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]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 50 mg/mL (130.81 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)

* "≥" 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 2.6161 mL 13.0806 mL 26.1613 mL
5 mM 0.5232 mL 2.6161 mL 5.2323 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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.54 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.54 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.76%

參考文獻(xiàn)
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(xiàn)

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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?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
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.

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產(chǎn)品名稱：
AT7519
目錄號：
HY-50940
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