AZD-7648|cas:2230820-11-6|西域试剂

AZD-7648,99.89%

产品编号：Bellancom-111783| CAS NO：2230820-11-6| 分子式：C₁₈H₂₀N₈O₂| 分子量：380.40

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-111783	￥1000.00	杭州北京（现货）
Bellancom-111783	￥1500.00	杭州北京（现货）
Bellancom-111783	￥2500.00	杭州北京（现货）
Bellancom-111783	￥4000.00	杭州北京（现货）
Bellancom-111783	￥6000.00	杭州北京（现货）

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AZD-7648

产品介绍

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。

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.

体外研究

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

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

Western Blot Analysis

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

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; p.o.; once daily for 5 days) induces tumour growth inhibition and tumour regression.

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

Animal Model:	Nude mice, A549 xenografts and NCI-H1299 xenografts
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.

体内研究

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

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

Animal Model:	Nude mice, A549 xenografts and NCI-H1299 xenografts
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.

体内研究

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

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

Animal Model:	Nude mice, A549 xenografts and NCI-H1299 xenografts
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (13.14 mM; ultrasonic and warming and heat to 80°C)

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
10 mM	0.2629 mL	1.3144 mL	2.6288 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；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