AZD2281 free base · Synonyms: Olaparib

Olaparib is a potent and orally active PARP inhibitor.

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

Target PARP Autophagy Mitophagy

Research area Cancer

Purity >99% Stock Inquire

Data Sheet SDS COA

AZD2281 structure

CAS No.: 763113-22-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 g	USD 384.00	BP-02084-50g	In stock	Get quote
100 g	USD 614.00	BP-02084-100g	In stock	Get quote
250 g	USD 1,230.00	BP-02084-250g	In stock	Get quote
500 g	USD 1,970.00	BP-02084-500g	In stock	Get quote
1000 g	USD 3,150.00	BP-02084-1000g	In stock	Get quote

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Description

Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively.

Biological activity

In Vitro Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30 100 nM. In Vivo Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out[1]. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors.

Identifiers

SMILES: FC1=CC=C(CC2=NNC(=O)C3=C2C=CC=C3)C=C1C(=O)N1CCN(CC1)C(=O)C1CC1
InChIKey: FDLYAMZZIXQODN-UHFFFAOYSA-N

Specifications

MW (average): 434.4628
Formula: C₂₄H₂₃FN₄O₃
CAS No.: 763113-22-0
Physical state: Solid
Color: White to 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 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91

[2]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58.

[3]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272.

[4]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351.

Same target

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Same research area

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