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Niraparib (tosylate)
$77 – $308
Products Details
Product 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].
Web ID
– HY-10619B
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C26H28N4O4S
Citations
– 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.|Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568.|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. 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.|J Clin Invest. 2019 Mar 1;129(3):1211-1228.|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.|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.|Sci Rep. 2021 Sep 27;11(1):19138.|Theranostics. 2020 Jul 25;10(21):9477-9494. |Uppsala University. Department of Pharmaceutical Biosciences. 2022 Feb.|J Oncol. 2022 Apr 5;2022:2800488.
References
– [1]Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.|[2]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.|[3]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.|[4]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.
CAS Number
– 1038915-73-9
Molecular Weight
– 492.59
Compound Purity
– 99.99
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
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : 1 mg/mL (heat to 50°C)
Target
– Apoptosis;PARP
Isoform
– PARP1;PARP2;PARP3;PARP4;TNKS1/PARP5A
Pathway
– Apoptosis;Cell Cycle/DNA Damage;Epigenetics
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
