Niraparib (tosylate)

Niraparib (tosylate)

• CAS Number: 1038915-73-9
• UNSPSC Description: Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].
• Target Antigen: Apoptosis; PARP
• Type: Reference compound
• Related Pathways: Apoptosis;Cell Cycle/DNA Damage;Epigenetics
• Applications: Cancer-programmed cell death
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/MK-4827-tosylate.html
• Purity: 99.99
• Solubility: DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : 1 mg/mL (heat to 50°C)
• Smiles: NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O.O=S(C5=CC=C(C)C=C5)(O)=O
• Molecular Weight: 492.59
• References & Citations: [1]Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.|[2]Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.|[3]Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.|[4]Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.J Med Chem. 2023 Mar 6.|J Mol Med (Berl). 2019 Aug;97(8):1183-1193.|Patent. US20210299137A1.|Adv Sci (Weinh). 2022 Oct;9(30):e2201210.|Am J Cancer Res. 2024 Jan 15;14(1):378-389.|Am J Pathol. 2024 Aug 19.|Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568.|bioRxiv. 2024 Jul 10:2024.07.09.602803.|BMC Cancer. 2022 Mar 23;22(1):312.|Cancer Cell. 2020 Dec 14;38(6):844-856.e7.|Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867.|Cancer Discov. 2017 Sep;7(9):984-998.|Cancer Lett. 8 November 2021.|Cancer Res Commun. 2024 May 20.|Cancer Res. 2022 Apr 26:canres.CAN-22-0742-E.2022.|Cancers (Basel). 2023 May 11, 15(10), 2708.|Carcinogenesis. 2020 May 14;41(3):345-357. |Cell Death Dis. 2020 Apr 6;11(4):219. |Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. |DNA Repair (Amst). 2019 Jan;73:64-70.|EBioMedicine. 2020 Sep;59:102923.|Elife. 2021 Jun 23;10:e69454.|Elife. 2022 Apr 27;11:e72464.|Faculty of Biology, University of Belgrade. 2019 Aug.|Front Oncol. 2021 Jul 9;11:681441.|HAL. archives-ouvertes. 2020 Dec 4.|Int J Biol Sci. 2020 Feb 21;16(8):1363-1375.|Int J Cancer. 2024 Sep 6.|J Clin Invest. 2019 Mar 1;129(3):1211-1228.|J Med Chem. 2024 Feb 22;67(4):2349-2368.|J Oncol. 2022 Apr 5;2022:2800488.|JCI Insight. 2023 Nov 8;8(21):e165268.|Life Sci Alliance. 2021 Oct 5;4(12):e202101144.|Materials Today Bio. 2020 Oct 22;8:100082.|medRxiv. 2020 Jan.|Mol Cancer Ther. 2023 Feb 10;MCT-22-0396.|Mol Pharm. 2021 Nov 3.|Nat Biomed Eng. 2023 Jul 24.|Nat Commun. 2022 Nov 19;13(1):7107.|Neurooncol Adv. 2024 Nov 19;6(1):vdae187.|NPJ Precis Oncol. 2021 Jun 9;5(1):49.|Nucl Med Biol. 2016 Dec;43(12):752-758. |Oncogene. 2022 Aug 6.|Patent. US20170226063A1.|Patent. US20180134664A1.|Patent. US20180362972A1.|Patent. US20190092732A1.|Patent. US20200078369A1|Patent. US20200129476A1|Patent. US20200148645A1|Patent. US20220048863A1.|Patent. US9932310B2.|PeerJ. 2023 Nov 29:11:e16314.|Research Square Preprint. 2022 Feb.|Research Square Preprint. 2024 Nov 06.|Sci Rep. 2021 Sep 27;11(1):19138.|Theranostics. 2020 Jul 25;10(21):9477-9494. |Uppsala University. Department of Pharmaceutical Biosciences. 2022 Feb.|Int J Biol Macromol. 2024 May 9:132275.|J Oncol. 2022 Apr 5;2022:2800488.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Launched