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Art. -Nr.: HY-183630

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AZD4956

AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC₅₀ value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors.

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CAS. Nr.: 3045469-78-8
Formel: C₂₈H₂₅Cl₂N₅O₄
Molecular Weight:566.44

Speicherung:

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

AZD4956 Chemical Structure

CAS. Nr.: 3045469-78-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Human pol θ

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

AZD4956 potently inhibits purified DNA polymerase theta (POLQ) in a biochemical assay with an IC₅₀ of < 3 nmol/L^[1].
AZD4956 inhibits microhomology-mediated end joining (MMEJ) in HEK-293T cells with an IC₅₀ of 3.4 nmol/L, phenocopying genetic POLQ deletion^[1].
AZD4956 exhibits significant synergistic combination effects with DNA-damaging agents such as Saruparib (HY-132167), preferentially in HRR-deficient cancer cells, whereas no significant synergy is observed with the non-DNA-damaging agent MMAE^[1].
AZD4956 (200 nM; 48 h), combined with Saruparib, significantly increases DNA damage markers (KAP1 phosphorylation, 53BP1 foci) and chromosomal aberrations in DLD-1 BRCA2+ cells^[1].

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

In Vivo

AZD4956 (100 mg/kg; BID) shows modest monotherapy antitumor activity in BRCA2-mutated TNBC PDX model (ST4316B) and PALB2-mutated TNBC PDX model (T298) in vivo^[1].
AZD4956 (100 mg/kg; BID) combined with Saruparib (HY-132167) (1 mg/kg; QD) achieves significant antitumor activity with TGI values of 110% in BRCA2-mutated mHSPC PDX model (C-901) and 101% in BRCA1-mutated TNBC PDX model (HBCx28) in vivo^[1].
AZD4956 (100 mg/kg; BID) combined with Saruparib (HY-132167) (1 mg/kg; QD) delays the acquisition of resistance in BRCA1-mutated TNBC PDX model (PDX179)^[1].
AZD4956 (3-50 mg/kg; BID) combined with Saruparib (HY-132167) (1 mg/kg; QD) exhibits dose-dependent enhanced antitumor activity in BRCA1-mutated TNBC PDX model (PDX127)^[1].

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

Animal Model:

Female immunocompromised mice bearing PDX127 (BRCA1m TNBC) PDX tumors were treated with AZD4956 at multiple doses in combination with saruparib.^[1]
Dosage:

AZD4956 3/10/25/50 mg/kg + saruparib 1 mg/kg
Administration:

AZD4956 twice daily (BID), saruparib once daily (QD); throughout the treatment period
Result:

Exhibited dose-dependent enhanced antitumor activity, with higher AZD4956 doses producing greater tumor growth inhibition and prolonged durable responses compared to saruparib monotherapy.
Increased micro-nucleated red blood cells in peripheral blood, indicating on-target activity of POLQ inhibition.

Chemical Information

CAS. Nr. 3045469-78-8
Molecular Weight 566.44
Formel C₂₈H₂₅Cl₂N₅O₄
SMILES

ClC1=CC=C(C#N)C(CN2C3=NC=NC(OC4(C)CC4)=C3N=C2C5=CC=CC(OCC[C@@H](C)C(O)=O)=C5Cl)=C1
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

Handling Instructions (2659 KB)

Verweise

[1]. Forment JV, et al. AZD4956, a potent and selective inhibitor of DNA polymerase theta, enhances the activity of DNA-damaging agents in HRR defective cellular backgrounds and improves efficacy of the new generation PARP1-selective inhibitor, saruparib. Cancer Res. 2026;86(7 Suppl):Abstract 230.

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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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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AZD4956

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

AZD4956 Related Classifications

HY-183630 Related Classifications