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  2. Cell Cycle/DNA Damage
  3. CDK
  4. AZD-5438

AZD-5438 是有效的 CDK1, CDK2, CDK9 抑制劑，IC50 值分別為 16 nM, 6 nM, 20 nM。AZD-5438 對 GSK3β，CDK5，CDK6 的抑制作用較弱。

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AZD-5438 Chemical Structure

AZD-5438 Chemical Structure

CAS No. : 602306-29-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥770
In-stock
1 mg ￥318
In-stock
5 mg ￥700
In-stock
10 mg ￥1105
In-stock
50 mg ￥4201
In-stock
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

  • 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

AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 [1].

IC50 & Target[1]

cdk2-cyclin E

6 nM (IC50)

cdk2-cyclin A

45 nM (IC50)

cdk5-p25

14 nM (IC50)

cdk1-cyclin B1

16 nM (IC50)

cdk9-cyclin T

20 nM (IC50)

cdk6-cyclin D3

21 nM (IC50)

cdk4-cyclin D1

449 nM (IC50)

cdk7-cyclin H

821 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.47 μM
Compound: AZD5438
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
HeLa IC50
0.73 μM
Compound: AZD5438
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
HeLa IC50
1.2 μM
Compound: 6; MMV676604
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
[PMID: 30647879]
LoVo IC50
0.63 μM
Compound: 6c, AZD-5438
Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs
[PMID: 18815031]
LoVo IC50
0.8 μM
Compound: 1, AZD-5438
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
[PMID: 18996007]
LoVo IC50
0.8 μM
Compound: 6
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
[PMID: 18986805]
MCF7 IC50
10.67 μM
Compound: AZD5438
Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
MDA-MB-231 IC50
7.2 μM
Compound: AZD5438
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
PC-3 IC50
0.36 μM
Compound: AZD5438
Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
體外研究
(In Vitro)

AZD5438 有效抑制細(xì)胞周期蛋白 E-cdk2、細(xì)胞周期蛋白 A-cdk2、細(xì)胞周期蛋白 B1-cdk1、p25-cdk5、細(xì)胞周期蛋白 D3-cdk6 和細(xì)胞周期蛋白 T-cdk9 的激酶活性 (IC50，6，45、16、21 和 20 nM)。AZD5438 有效抑制細(xì)胞周期蛋白 E-cdk2、細(xì)胞周期蛋白 A-cdk2、細(xì)胞周期蛋白 B1-cdk1、p25-cdk5、細(xì)胞周期蛋白 D3-cdk6 和細(xì)胞周期蛋白 T-cdk9 的激酶活性 (IC50，6，45、16、21 和 20 nM)。與許多其他 cdk 抑制劑一樣，AZD5438 還在體外抑制 p25-cdk5 和糖原合酶激酶 3β 的激酶活性 (IC50 分別為 14 和 17 nM)[1]。AZD5438 顯著增強(qiáng) NSCLC 細(xì)胞的細(xì)胞放射敏感性。AZD5438 聯(lián)合放療也可增強(qiáng)腫瘤生長延遲，增強(qiáng)因子范圍為 1.2-1.7[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

AZD5438 (50 mg/kg，每日兩次或 75 mg/kg，口服) 抑制人腫瘤異種移植物的生長。在體內(nèi)，AZD5438 降低活躍循環(huán)細(xì)胞的比例。對 AZD5438 處理的 SW620 異種移植物的進(jìn)一步藥效學(xué)分析表明，有效劑量的 AZD5438 (>40% 腫瘤生長抑制) 在單次口服劑量后可維持對生物標(biāo)志物 (如磷酸 pRbSer249/Thr252) 的抑制長達(dá) 16 小時[1]。

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

371.46

Formula

C18H21N5O2S
CAS 號
性狀

固體

顏色

White to light yellow

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 : 100 mg/mL (269.21 mM; 超聲助溶; 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6921 mL 13.4604 mL 26.9208 mL
5 mM 0.5384 mL 2.6921 mL 5.3842 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 (6.73 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 (6.73 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: 99.85%

參考文獻(xiàn)
Cell Assay
[1]

AZD5438 is tested against solid tumor cell lines as previously described. Briefly, cells are incubated for 48 h with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2'-deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 h. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

All human tumor xenografts except HX147 are established by s.c. injecting 100 μL of tumor cells (between 1×106 and 1×107 cells mixed 1:1 with Matrigel). HX147 tumors are derived from fragment implants (1 mm3 pieces) from tumors taken from mice initially implanted s.c. with 1×107 cells. These tumor fragments are passaged in mice thrice before implant for antitumor work. Tumors are measured up to three times per week with calipers, tumor volumes are calculated, and the data are plotted as geometric mean for each group versus time, as previously described. Animals are randomized into treatment groups (typically n=10) when tumors reach a mean size of approximately >0.2 cm3 and >0.5 cm3 for mice and rats, respectively. AZD5438 is prepared in hydroxy-propyl-methyl-cellulose. Animals are given either AZD5438 (37.5-75 mg/kg) or vehicle control once or twice daily by oral gavage for appr 3 wk in each case. Tumor volume and percentage tumor growth inhibition (% TGI) are calculated as described previously. Statistical analysis of any change in tumor volume is carried out using a standard t test (P<0.05 is considered to be statistically significant).

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 2.6921 mL 13.4604 mL 26.9208 mL 67.3020 mL
5 mM 0.5384 mL 2.6921 mL 5.3842 mL 13.4604 mL
10 mM 0.2692 mL 1.3460 mL 2.6921 mL 6.7302 mL
15 mM 0.1795 mL 0.8974 mL 1.7947 mL 4.4868 mL
20 mM 0.1346 mL 0.6730 mL 1.3460 mL 3.3651 mL
25 mM 0.1077 mL 0.5384 mL 1.0768 mL 2.6921 mL
30 mM 0.0897 mL 0.4487 mL 0.8974 mL 2.2434 mL
40 mM 0.0673 mL 0.3365 mL 0.6730 mL 1.6825 mL
50 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.3460 mL
60 mM 0.0449 mL 0.2243 mL 0.4487 mL 1.1217 mL
80 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6730 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：
AZD-5438
目錄號：
HY-10012
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