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

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.

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AZD-7648

AZD-7648 構造式

CAS 番号 : 2230820-11-6

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AZD-7648 関連抗体

Top Publications Citing Use of Products

ATM/ATR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ATM ATR TRRAP

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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製品説明

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)

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]
B16-F10 IC50
11.4 μM
Compound: AZD-7648
Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
[PMID: 38587857]
B16-F10 IC50
33.6 μM
Compound: AZD-7648
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38587857]
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]
CT26 IC50
18.8 μM
Compound: AZD-7648
Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38587857]
CT26 IC50
6.74 μM
Compound: AZD-7648
Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
[PMID: 38587857]
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]
HCT-116 IC50
38.08 nM
Compound: 4; AZD7648
Inhibition of colony formation in human HCT-116 cells preincubated with compound for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 7 days by crystal violet staining based chemiluminescence assay
Inhibition of colony formation in human HCT-116 cells preincubated with compound for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 7 days by crystal violet staining based chemiluminescence assay
[PMID: 38117951]
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]
Jurkat IC50
0.09 μM
Compound: AZD-7648
Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay
[PMID: 38587857]
Jurkat IC50
12.3 μM
Compound: AZD-7648
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38587857]
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]
体外実験

AZD7648 (GMP) (0-30 μM) is a potent radiosensitizer[1].
AZD7648 (GMP) (3 μM) increases sensitivity to Doxorubicin (HY-15142A)[1].
AZD7648 (0.6 μM) enhances the activity of PARP inhibitor Olaparib (HY-10162)[1].

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

AZD-7648 関連抗体

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).
体内実験

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

MedChemExpress (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.
臨床実験
分子量

380.40

分子式

C18H20N8O2
CAS 番号
SMILES

CC1=CC2=NC=NN2C=C1NC3=NC=C(N(C)C(N4C5CCOCC5)=O)C4=N3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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AZD-7648 Related Classifications

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Keywords:

AZD-7648 (GMP)2230820-11-6DNA-PKATM/ATRPI3KApoptosisDNA-dependent protein kinaseAtaxia telangiectasia mutatedATM and RAD3 relatedPhosphoinositide 3-kinaseA549OAW42antitumorGMPInhibitorinhibitorinhibit

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製品番号:
HY-111783G
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