AZD-5305 free base · Synonyms: AZD 5305 · AZD5305

AZD5305 is a potent, selective and oral active PARP inhibitor.

For research use only. Not for human or veterinary use.

Target PARP

Research area Cancer

Purity >99% Stock Inquire

Data Sheet SDS COA

AZD-5305 structure

CAS No.: 2589531-76-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 588.00	BP-02031-500mg	In stock	Get quote
1 g	USD 792.00	BP-02031-1g	In stock	Get quote
2 g	USD 1,396.00	BP-02031-2g	In stock	Get quote
3 g	USD 2,000.00	BP-02031-3g	In stock	Get quote
5 g	USD 2,800.00	BP-02031-5g	In stock	Get quote
10 g	Inquire	BP-02031-10g	In stock	Inquire

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Description

AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models.

Biological activity

n Vitro Saruparib (AZD5305) (0.1 nM-100 μM) inhibits PARylation in A549 WT cells by selectively blocking PARP1 enzymatic activity with an IC50 value of 2.3 nM. AZD5305 (0.1 nM-100 μM; A549 WT cells) is a potent and selective trapper of PARP1 in a dose-dependent manner by single digit nanomolar concentrations. AZD5305 (0.1 nM-100 μM; 48 h; DLD1 WT and DLD1 BRCA2-/-) has anti-proliferative activity and targets cancer cells with HRR-deficiency, inducing DNA damage accumulation and cell-cycle arrest. 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.

Identifiers

SMILES: O=C(C1=NC=C(N2CCN(CC3=CC(N4)=C(N=C3)C=C(CC)C4=O)CC2)C=C1)NC
InChIKey: WQAVGRAETZEADU-UHFFFAOYSA-N

Specifications

MW (average): 406.4808
Formula: C₂₂H₂₆N₆O₂
CAS No.: 2589531-76-8
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 25 mg/mL

Documents

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.

[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.

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Same research area

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