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Chemical Structure| 1821428-35-6 Chemical Structure| 1821428-35-6

Structure of AZD0156
CAS No.: 1821428-35-6

Chemical Structure| 1821428-35-6

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AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.

Synonyms: AZD0156

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Product Details of AZD0156

CAS No. :1821428-35-6
Formula : C26H31N5O3
M.W : 461.56
SMILES Code : O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3
Synonyms :
AZD0156
MDL No. :MFCD30470661
InChI Key :AOTRIQLYUAFVSC-UHFFFAOYSA-N
Pubchem ID :118502708

Safety of AZD0156

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZD0156

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • ATM

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS cells 2nM 1 h To assess cell sensitivity to proton treatment. PMC8260463
U251 ATRXKO cells 30 nM ATRX-deficient cells exhibited significant radiation sensitivity at 30 nM of AZD0156. PMC8759735
U251 ATRXKO cells 1 µM 4 hours To evaluate the effect of AZD0156 on ATM inhibition in ATRX-deficient cells, results showed reduced levels of pATM and gH2AX. PMC8759735
D54-ATMR cells 10 µM 70 minutes To evaluate the effect of AZD0156 on the ATM inhibition reporter, results showed a sustained increase in ATM inhibition signal. PMC8759735
U251 ATRXKO cells 30 nM 1 hour To evaluate the radiosensitization effect of AZD0156 on ATRX-deficient glioma cells, results showed that AZD0156 significantly enhanced the sensitivity of ATRX-deficient cells to radiation PMC8759735
SJ-GBM2 cells 30 nM 1 hour To evaluate the radiosensitization effect of AZD0156 on ATRX-deficient glioma cells, results showed that AZD0156 significantly enhanced the sensitivity of ATRX-deficient cells to radiation PMC8759735
U251 ATRXKO cells 1 µM 4 hours To evaluate the effect of AZD0156 on ATRX-deficient cells, results showed that AZD0156 inhibited ATM kinase activity. PMC8759735
D54-ATMR cells 10 µM and 10 nM 70 minutes To evaluate the effect of AZD0156 and AZD1390 on ATM inhibition, results showed that AZD0156 and AZD1390 had a sustained inhibitory effect on ATM in vitro. PMC8759735
MOC2 cells 50 nM 24 hours AZD0156 (50 nM) increased Ifnβ expression in MOC2 cells following 8 Gy RT. PMC10510866
B78 cells 50 nM 24 hours AZD0156 (50 nM) increased Ifnβ expression in B78 cells following 12 Gy RT. PMC10510866
SCC6 cells 50 nM 24 hours AZD0156 (50 nM) increased Ifnβ expression in SCC6 cells following 8 Gy RT. PMC10510866
TFK-1 cells 2 μM 8 hours Inhibition of TET1 protein expression PMC11653675
EGI-1 cells 2 μM 8 hours Inhibition of TET1 protein expression PMC11653675
ALT neuroblastoma cell lines 100 nM To evaluate the sensitivity of AZD0156 to TMZ+SN-38, results showed that AZD0156 significantly enhanced the sensitivity of ALT neuroblastoma cell lines to TMZ+SN-38 PMC9208664
Telomerase-positive neuroblastoma cell lines 100 nM To evaluate the sensitivity of AZD0156 to TMZ+SN-38, results showed that telomerase-positive cell lines had a heterogeneous response to AZD0156 PMC9208664

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice MC-BR-BTY-0030 Intraperitoneal injection 10 mg/kg one hour prior to and 24 following irradiation To enhance the efficacy of proton Bragg peak irradiation. PMC8260463
Mice Balb/c nude mice Oral 10 mg/kg enhanced efficacy of low-dose CFI-400945 when combined with AZD0156 PMC11369621
Mice ATRX-deficient orthotopic murine brain tumor model Intraperitoneal injection 10 mg/kg 3-4 times per week for 2 weeks To evaluate the effect of ATM inhibitor AZD0156 on the survival of ATRX-deficient glioma mice, results showed that AZD0156 significantly extended the median survival of mice. PMC8759735
Mice ATRX-deficient orthotopic GBM model Intraperitoneal injection 10 mg/kg Every 3-4 days for two weeks Combination treatment with AZD0156 and radiation significantly extended the survival of mice with ATRX-deficient GBM models. PMC8759735
Mice ATRX-deficient GBM neurosphere model Intraperitoneal injection 10 mg/kg 4 times per week for 2 weeks To evaluate the radiosensitizing effect of AZD0156 on ATRX-deficient tumors, results showed a significant increase in median survival. PMC8759735
Mice ATRX-deficient glioma model Intraperitoneal injection 10 mg/kg every 3-4 days for two weeks, total of 4 treatments To evaluate the therapeutic effect of AZD0156 on the ATRX-deficient glioma model, results showed that AZD0156 significantly extended the survival of mice PMC8759735
C57BL/6 mice MOC2 and B78 tumor models Oral 10 mg/kg once daily for five consecutive days Combination of AZD0156 with radiotherapy significantly suppressed tumor growth in MOC2 and B78 models and improved mouse survival. PMC10510866
Mice ALT neuroblastoma xenograft models Oral 20 mg/kg Once daily for 14 days To evaluate the effect of AZD0156 in combination with TMZ+IRN, results showed that AZD0156 significantly extended event-free survival in ALT xenograft models PMC9208664

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.67mL

4.33mL

2.17mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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