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

AZD-7648 (GMP) 是 GMP 级别的 AZD-7648 (HY-111783)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。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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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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 (IC50)

ATM

17.93 (IC50)

DNA-PKcs

91.3 nM (IC50)

体外研究
(In Vitro)

AZD7648 (GMP) (0-30 μM) 是一种有效的放射增敏剂[1]
AZD7648 (GMP) (3 μM) 可增加对 Doxorubicin (HY-15142A) 的敏感性[1]
AZD7648 (GMP) (0.6 μM) 增强 PARP 抑制剂 Olaparib (HY-10162) 的活性[1]

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

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.

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).
体内研究
(In Vivo)

AZD-7648 (GMP) (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
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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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产品名称:
AZD-7648
目录号:
HY-111783G
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