Art. -Nr.: HY-111783G

AZD-7648 (GMP)

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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CAS. Nr.: 2230820-11-6
Formel: C₁₈H₂₀N₈O₂
Molecular Weight:380.40

Speicherung:

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

Data Sheet (276 KB)

AZD-7648 (GMP) Chemical Structure

CAS. Nr.: 2230820-11-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kγ

1.37 (IC₅₀)

ATM

17.93 (IC₅₀)

DNA-PKcs

91.3 nM (IC₅₀)

Alle ATM/ATR Isoform-spezifische Produkte anzeigen :

Alle PI3K Isoform-spezifische Produkte anzeigen :

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]

In Vitro

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.

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).

In Vivo

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2230820-11-6
Molecular Weight 380.40
Formel C₁₈H₂₀N₈O₂
SMILES

CC1=CC2=NC=NN2C=C1NC3=NC=C(N(C)C(N4C5CCOCC5)=O)C4=N3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fok JHL, et al. AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity. Nat Commun. 2019 Nov 7;10(1):5065. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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AZD-7648 (GMP)

Alle ATM/ATR Isoform-spezifische Produkte anzeigen

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

AZD-7648 (GMP) Related Classifications

HY-111783G Related Classifications