Olaparib Synthesis Route

Olaparib Synthesis

Olaparib (Synonyms: 4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one)

Many of the products generated by alkylating agents on DNA can be efficiently repaired by normal base excision repair (BER).1 Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in BER.2 Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM).3 It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.

Olaparib

A PARP inhibitor

Item No. AB48261
CAS No. 763113-22-0
Purity: 98%

100mg

＄6.00

250mg

＄7.00

＄15.00

＄65.00

10g

＄113.00

100g

＄922.00

Quantity

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Olaparib Synthetic Route

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1.1: sodium methylate / methanol / 2 h / 0 - 20 °C / Inert atmosphere
1.2: 0.5 h / Inert atmosphere
2.1: triethylamine / tetrahydrofuran / 48 h / 0 - 20 °C / Inert atmosphere
3.1: sodium hydroxide / water / 24 h / 90 °C / Inert atmosphere
4.1: hydrazine hydrate / 72 h / 70 °C / Inert atmosphere
5.1: triethylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere
5.2: 72 h / 50 °C / Inert atmosphere
6.1: hydrogenchloride / water; ethanol / 20 °C / Inert atmosphere
7.1: triethylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere
7.2: 72 h / 20 °C / Inert atmosphere

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References

1.Journal of Medicinal Chemistry, 2015, vol. 58, # 21, p. 8683 - 8693

2.Rowe, B.P., and Glazer, P.M. Emergence of rationally designed therapeutic strategies for breast cancer targeting DNA repair mechanisms. Breast Cancer Res. 12(2), 1-11 (2010).

3.Davar, D., Beumer, J.H., Hamieh, L., et al. Role of PARP inhibitors in cancer biology and therapy. Curr. Med. Chem. 19(23), 3907-3921 (2012).

4.Menear, K.A., Adcock, C., Boulter, R., 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. 51(20), 6581-6591 (2008).

5.Yuan, Y., Liao, Y.M., Hsueh, C.T., et al. Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011).

6.Plummer, R. Poly(ADP-ribose) polymerase inhibition: A new direction for BRCA and triple-negative breast cancer? Breast Cancer Res. 13(4), 1-6 (2011).

7.Javle, M., and Curtin, N.J. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther. Adv. Med. Oncol. 3(6), 257-267 (2011).