2143107-55-3
2143107-55-3
Chemical Structure
Olaparib-d4-1
Synonym(s): AZD2281-d4-1;KU0059436-d4-1
- CAS No.: 2143107-55-3
- Formula:C24H19D4FN4O3
- Molecular Weight:438.49
IUPAC Name: 4-(3-(4-(cyclopropane-1-carbonyl-d4)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
InChIKey: FDLYAMZZIXQODN-KXGHAPEVSA-N
SMILES: O=C(N1CCN(CC1)C(C2=C(C=CC(CC(C3=C4C=CC=C3)=NNC4=O)=C2)F)=O)C5C([2H])(C5([2H])[2H])[2H]
Biological Activity: Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Olaparib-d4-1 | 98.82% | Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. | ||||||||||||||||||||
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Olaparib (Standard) | 99.48% | Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. | ||||||||||||||||||||
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Olaparib-d5 | 99.37% | Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. | ||||||||||||||||||||
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Olaparib-d8 | 99.88% | Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. | ||||||||||||||||||||
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Olaparib-d4-2 | Olaparib-d4-2 is the deuterium labeled Olaparib (HY-10162). Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. Olaparib cannot cross the intact blood-brain barrier (BBB). | |||||||||||||||||||||
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Olaparib | 99.98% | Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. Olaparib cannot cross the intact blood-brain barrier (BBB). | ||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
- [2]. 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 [Content Brief]
- [3]. 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. [Content Brief]
- [4]. 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. [Content Brief]
