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

AZD-7648 是一种具有选择性的口服有效 DNA-PK 抑制剂，IC50 值为 0.6 nM, AZD-7648 诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。

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AZD-7648 Chemical Structure

AZD-7648 Chemical Structure

CAS No. : 2230820-11-6

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规格 价格 是否有货 数量
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
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

AZD-7648 相关抗体

Top Publications Citing Use of Products

查看 ATM/ATR 亚型特异性产品:

查看所有亚型
ATM ATR

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1]

PI3Kγ

1.37 μM (IC50)

ATM

17.93 μM (IC50)

DNA-PKcs

91.3 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.091 μM
Compound: Example 16; AZD7648
Inhibition of DNA-PK in human A549 cells assessed as reduction in irradiation-induced autophosphorylation at S2056 residue preincubated for 1 hr followed by 8 Gy irradiation and measured after 1 hr by ELISA
Inhibition of DNA-PK in human A549 cells assessed as reduction in irradiation-induced autophosphorylation at S2056 residue preincubated for 1 hr followed by 8 Gy irradiation and measured after 1 hr by ELISA
[PMID: 31851518]
CHO IC50
> 198 μM
Compound: Example 16; AZD7648
Inhibition of human ERG stably expressed in CHO cells at -90 mV holding potential by electrophysiological assay
Inhibition of human ERG stably expressed in CHO cells at -90 mV holding potential by electrophysiological assay
[PMID: 31851518]
HCT-116 IC50
19.5 μM
Compound: AZD-7648
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay
[PMID: 35468512]
HCT-116 IC50
35.3 μM
Compound: AZD-7648
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35468512]
HeLa IC50
0.6 nM
Compound: Example 16; AZD7648
Inhibition of human HeLa cell-derived full length DNA-PK catalytic subunit using fluorescein-EPPLSQEAFADLWKK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins TR-FRET assay
Inhibition of human HeLa cell-derived full length DNA-PK catalytic subunit using fluorescein-EPPLSQEAFADLWKK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins TR-FRET assay
[PMID: 31851518]
HT-29 IC50
> 29 μM
Compound: Example 16; AZD7648
Inhibition of ATR in human HT-29 cells assessed as reduction in 4NQO-induced CHK1 phosphorylation at S345 residue preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst staining-based imaging analysis
Inhibition of ATR in human HT-29 cells assessed as reduction in 4NQO-induced CHK1 phosphorylation at S345 residue preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst staining-based imaging analysis
[PMID: 31851518]
HT-29 IC50
17.9 μM
Compound: Example 16; AZD7648
Inhibition of ATM in human HT-29 cells assessed as reduction in irradiation-induced autophosphorylation at Ser1981 residue preincubated for 1 hr followed by 6 Gy irradiation and measured after 1 hr by Hoechst staining-based imaging analysis
Inhibition of ATM in human HT-29 cells assessed as reduction in irradiation-induced autophosphorylation at Ser1981 residue preincubated for 1 hr followed by 6 Gy irradiation and measured after 1 hr by Hoechst staining-based imaging analysis
[PMID: 31851518]
MDA-MB-231 IC50
> 30 μM
Compound: Example 16; AZD7648
Inhibition of mTOR/PI3Kalpha in human MDA-MB-231 cells assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Hoechst staining-based imaging analysis
Inhibition of mTOR/PI3Kalpha in human MDA-MB-231 cells assessed as reduction in AKT phosphorylation at S473 residue measured after 2 hrs by Hoechst staining-based imaging analysis
[PMID: 31851518]
MDA-MB-468 IC50
> 30 μM
Compound: Example 16; AZD7648
Inhibition of PI3Kbeta in human MDA-MB-468 cells assessed as reduction in AKT phosphorylation at T208 residue measured after 2 hrs by QuantaBlu substrate based fluorescence assay
Inhibition of PI3Kbeta in human MDA-MB-468 cells assessed as reduction in AKT phosphorylation at T208 residue measured after 2 hrs by QuantaBlu substrate based fluorescence assay
[PMID: 31851518]
体外研究
(In Vitro)

AZD7648 (0-30 μM) 是一种有效的放射增敏剂[1]。
AZD7648 (3 μM) 可增加对阿霉素的敏感性[1]。
AZD7648 (0.6 μM) 增强 PARP 抑制剂 Olaparib 的活性[1]。

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

AZD-7648 相关抗体:

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.
体内研究
(In Vivo)

AZD-7648（100 mg/kg；口服；每天一次，连续 5 天）可抑制肿瘤生长并抑制肿瘤消退[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 号
性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 5.83 mg/mL (15.33 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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。-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。

  • 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

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂： 0.5% HPMC/0.1% Tween-80 in Saline water

    Solubility: 10 mg/mL (26.29 mM); 悬浊液; 超声助溶

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: 99.86%

COA (289 KB) HNMR (263 KB) LCMS (264 KB)

产品使用指南 (1538 KB)
参考文献

AZD-7648 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。-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
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.

Keywords:

AZD-76482230820-11-6AZD7648AZD 7648DNA-PKATM/ATRPI3KApoptosisDNA-dependent protein kinaseAtaxia telangiectasia mutatedATM and RAD3 relatedPhosphoinositide 3-kinaseA549OAW42antitumorInhibitorinhibitorinhibit

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目录号：
HY-111783
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