Basic information Safety Supplier Related

AZD-5305

Basic information Safety Supplier Related

AZD-5305 Basic information

Product Name:
AZD-5305
Synonyms:
  • 2-Pyridinecarboxamide, 5-[4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methyl-
  • AZD-5305
  • 5-[4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methylpicolinamide
  • repair,AZD5305,Inhibitor,poly ADP ribose polymerase,DNA,AZD-5305,PARP,inhibit,pathway,synthetic,AZD 5305,lethality
  • 5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)-N-methylpicolinamide
  • Saruparib (AZD5305)
  • saruparib
  • 5-{4-[(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide
CAS:
2589531-76-8
MF:
C22H26N6O2
MW:
406.48
Product Categories:
  • api
Mol File:
2589531-76-8.mol
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AZD-5305 Chemical Properties

Boiling point:
702.6±60.0 °C(Predicted)
Density 
1.246±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 41.67 mg/mL (102.51 mM; Need ultrasonic)
pka
11.26±0.40(Predicted)
form 
Solid
color 
Off-white to light yellow
InChIKey
WQAVGRAETZEADU-UHFFFAOYSA-N
SMILES
C1(C(NC)=O)=NC=C(N2CCN(CC3=CC4=C(N=C3)C=C(CC)C(=O)N4)CC2)C=C1
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AZD-5305 Usage And Synthesis

Uses

Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair[1][2].

in vivo

Saruparib (AZD5305) (0.01-0.3 mg/kg; p.o.; daily, for 35 d; female Han Wistar rats) demonstrates sustained antitumor activity in BRCAm xenograft and PDX models in vivo[1].

Animal Model:Female Han Wistar rats with BRCAm xenograft and PDX models (12-13 weeks of age)[1]
Dosage:0.01, 0.03, 0.1, and 0.3 mg/kg
Administration:Oral administration; daily, for 35 days
Result:Had antitumor efficacy in a dose-dependent manner.

IC 50

PARP1: 3 nM (IC50); PARP2: 1400 nM (IC50)

References

[1] Illuzzi G, et, al. Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736. DOI:10.1158/1078-0432.CCR-22-0301
[2] Johannes JW, et, al. Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs. J Med Chem. 2021 Oct 14;64(19):14498-14512. DOI:10.1021/acs.jmedchem.1c01012

AZD-5305Supplier

Changsha Fuzhen Biotechnology Co.，LTD Gold
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0731-13823398 15111215862
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Bayee Biotech (Anqing) Co., Ltd.
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0556-5032306 18917961636
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 18971495150;
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sales@sun-shinechem.com
Shanghai Topbiochem Technology Co., Ltd
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021-58170097
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info@topbiochem.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
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AZD-5305(2589531-76-8)Related Product Information