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Chemical Structure| 2589531-76-8 Chemical Structure| 2589531-76-8

Structure of Saruparib
CAS No.: 2589531-76-8

Chemical Structure| 2589531-76-8

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AZD-5305 is a potent and highly selective PARP1 inhibitor. AZD5305 dosed at 0.1mg/kg QD or higher for 35 days delivered about 90% regression in the BRCA1m triple-negative breast cancer (TNBC) xenograft model MDA-MB-436.

Synonyms: AZD5305

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Product Details of Saruparib

CAS No. :2589531-76-8
Formula : C22H26N6O2
M.W : 406.48
SMILES Code : O=C(C1=NC=C(N2CCN(CC3=CC(N4)=C(N=C3)C=C(CC)C4=O)CC2)C=C1)NC
Synonyms :
AZD5305
MDL No. :MFCD34471686
InChI Key :WQAVGRAETZEADU-UHFFFAOYSA-N
Pubchem ID :155586901

Safety of Saruparib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of Saruparib

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 PARP1-KO cells 653 nM 1 hour To evaluate the ability of AZD5305 to inhibit PARylation in PARP1-deficient cells, results showed a significant increase in IC50 value. PMC9623235
A549 WT cells 2.3 nM 1 hour To assess the ability of AZD5305 to inhibit the catalytic activity of PARP, results showed AZD5305 effectively inhibited PARylation in A549 WT cells. PMC9623235
U-2 OS cells 10 μM 16 hours Evaluate the stabilizing effect of PARPi on PARP1 L713F-GFP and PARP2 L269A-mCherry biosensors PMC11986510
DLD-1 BRCA2-/- cells 0.4 nM 8-13 days To evaluate the antiproliferative effects of AZD5305 in BRCA2-deficient cells, results showed an IC50 of 0.4 nmol/L. PMC9623235

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Patient-derived xenograft (PDX) model Oral gavage 1 or 10 mg/kg Daily administration for 28 days To evaluate the efficacy of AZD5305 in HRD uLMS PDX models, results showed that AZD5305 induced rapid and sustained complete responses even in PARPi-resistant PDX containing PRKDC mutations. PMC10157936

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0.25mL

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4.92mL

2.46mL

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