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  2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. DNA-PK ATM/ATR PI3K Apoptosis
  4. AZD-7648

AZD-7648 是一種具有選擇性的口服有效 DNA-PK 抑制劑，IC50 值為 0.6 nM, AZD-7648 誘導(dǎo)細(xì)胞凋亡 (apoptosis)，具有抗腫瘤活性。

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AZD-7648 Chemical Structure

AZD-7648 Chemical Structure

CAS No. : 2230820-11-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥880
In-stock
5 mg ￥800
In-stock
10 mg ￥1100
In-stock
25 mg ￥2200
In-stock
50 mg ￥3250
In-stock
100 mg ￥5000
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

查看 ATM/ATR 亞型特異性產(chǎn)品:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity[1].

IC50 & Target

DNA-PKcs

91.3 nM (IC50)

PI3Kγ

1.37 μM (IC50)

ATM

17.93 μM (IC50)

體外研究
(In Vitro)

AZD7648 (0-30 μM) is a potent radiosensitizer[1].
AZD7648 (3 μM) increases sensitivity to doxorubicin[1].
AZD7648 (0.6 μM) enhances the activity of PARP inhibitor olaparib[1].

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

Western Blot Analysis[1]

Cell Line: IR (ionizing radiation)-treated A549 cells or OAW42 cells treated with doxorubicin
Concentration: 0.03, 0.1, 0.3, 1, 3, 10 and 30 μM for A549; 3 μM for OAW42
Incubation Time: 1 h for A549; 0.5, 2, 4, 8 and 16 h for OAW42
Result: Potently inhibited DNA-PKcs autophosphorylation at Ser2056. Downregulated pDNA-PKcs Ser2056, γH2AX Ser139 and pRPA32 Ser4/Ser8 phosphorylation at early time points (at 30?min, 2?h and 4?h). Resulted in increased levels of γH2AX and the apoptosis marker cleaved PARP1 compared with doxorubicin treatment alone at later time points (8 and 16?h).

Cell Cycle Analysis[1]

Cell Line: IR (ionizing radiation)-treated A549 cells or A549 cells
Concentration: 0-30 μM
Incubation Time: 48 h
Result: Arrested cell cycle at G2/M phase.
體內(nèi)研究
(In Vivo)

AZD-7648 (100 mg/kg; p.o.; once daily for 5 days) induces tumour growth inhibition and tumour regression[1].

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

Animal Model: Nude mice, A549 xenografts and NCI-H1299 xenografts[1]
Dosage: 100 mg/kg
Administration: Oral administration, once daily for 5 days
Result: Induced tumour growth inhibition in combination with IR in A549 xenografts and induced tumour regression in combination with IR in NCI-H1299 xenografts.
Clinical Trial
分子量

380.40

Formula

C18H20N8O2
CAS 號(hào)
性狀

固體

顏色

White to yellow

運(yùn)輸條件

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

DMSO 中的溶解度 : 5.83 mg/mL (15.33 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6288 mL 13.1441 mL 26.2881 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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(dòng)物實(shí)驗(yàn)：

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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(qǐng)依序添加每種溶劑： 0.5% HPMC/0.1% Tween-80 in Saline water

    Solubility: 10 mg/mL (26.29 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.86%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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 2.6288 mL 13.1441 mL 26.2881 mL 65.7203 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL 13.1441 mL
10 mM 0.2629 mL 1.3144 mL 2.6288 mL 6.5720 mL
15 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 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-7648
目錄號(hào)：
HY-111783
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