Niraparib HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201916

CAS#: 1038915-64-8 (HCl)

Description: Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Chemical Structure

Niraparib HCl
CAS# 1038915-64-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 201916
Name: Niraparib HCl
CAS#: 1038915-64-8 (HCl)
Chemical Formula: C19H21ClN4O
Exact Mass: 356.1404
Molecular Weight: 356.854
Elemental Analysis: C, 63.95; H, 5.93; Cl, 9.93; N, 15.70; O, 4.48

Size Price Shipping out time Quantity
100mg USD 750 2 Weeks
200mg USD 1150 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2950 2 Weeks
2g USD 4950 2 Weeks
5g USD 7450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

Niraparib HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 1038915-73-9 (tosylate)   1038915-60-4 (free base)   1038915-64-8 (HCl)   1613220-15-7 (tosylate hydrate)   1038915-58-0    

Synonym: MK4827; MK 4827; MK4827; Niraparib; Niraparib HCl; Niraparib hydrochloride; Zejula.

IUPAC/Chemical Name: (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride


InChi Code: InChI=1S/C19H20N4O.ClH/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);1H/t14-;/m1./s1

SMILES Code: O=C(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12)N.[H]Cl

Light yellow solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 356.854 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Krens S, van der Meulen E, Jansman FGA, Burger DM, van Erp NP. Quantification of cobimetinib, cabozantinib, dabrafenib, niraparib, olaparib, vemurafenib, regorafenib and its metabolite regorafenib M2 in human plasma by UPLC-MS/MS. Biomed Chromatogr. 2019 Nov 22:e4758. doi: 10.1002/bmc.4758. [Epub ahead of print] PubMed PMID: 31758580.

2: Gallagher JR, Heap KJ, Carroll S, Travers K, Harrow B, Westin SN. Real-world adverse events with niraparib 200 mg/day maintenance therapy in ovarian cancer: a retrospective study. Future Oncol. 2019 Dec;15(36):4197-4206. doi: 10.2217/fon-2019-0471. Epub 2019 Nov 11. PubMed PMID: 31707856.

3: Ji Y, Wang Q, Zhao Q, Zhao S, Li L, Sun G, Ye L. Autophagy suppression enhances DNA damage and cell death upon treatment with PARP inhibitor Niraparib in laryngeal squamous cell carcinoma. Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568. doi: 10.1007/s00253-019-10148-y. Epub 2019 Nov 4. PubMed PMID: 31686145.

4: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from PubMed PMID: 31643655.

5: Gourd E. Niraparib improves progression-free survival in ovarian cancer. Lancet Oncol. 2019 Nov;20(11):e615. doi: 10.1016/S1470-2045(19)30631-X. Epub 2019 Oct 3. PubMed PMID: 31587884.

6: González-Martín A, Pothuri B, Vergote I, DePont Christensen R, Graybill W, Mirza MR, McCormick C, Lorusso D, Hoskins P, Freyer G, Baumann K, Jardon K, Redondo A, Moore RG, Vulsteke C, O'Cearbhaill RE, Lund B, Backes F, Barretina-Ginesta P, Haggerty AF, Rubio-Pérez MJ, Shahin MS, Mangili G, Bradley WH, Bruchim I, Sun K, Malinowska IA, Li Y, Gupta D, Monk BJ; PRIMA/ENGOT-OV26/GOG-3012 Investigators. Niraparib in Patients with Newly Diagnosed Advanced Ovarian Cancer. N Engl J Med. 2019 Sep 28. doi: 10.1056/NEJMoa1910962. [Epub ahead of print] PubMed PMID: 31562799.

7: Matulonis UA, Walder L, Nøttrup TJ, Bessette P, Mahner S, Gil-Martin M, Kalbacher E, Ledermann JA, Wenham RM, Woie K, Lau S, Marmé F, Casado Herraez A, Hardy-Bessard AC, Banerjee S, Lindahl G, Benigno B, Buscema J, Travers K, Guy H, Mirza MR. Niraparib Maintenance Treatment Improves Time Without Symptoms or Toxicity (TWiST) Versus Routine Surveillance in Recurrent Ovarian Cancer: A TWiST Analysis of the ENGOT-OV16/NOVA Trial. J Clin Oncol. 2019 Dec 1;37(34):3183-3191. doi: 10.1200/JCO.19.00917. Epub 2019 Sep 16. PubMed PMID: 31518175; PubMed Central PMCID: PMC6881097.

8: Mirza MR, Åvall Lundqvist E, Birrer MJ, dePont Christensen R, Nyvang GB, Malander S, Anttila M, Werner TL, Lund B, Lindahl G, Hietanen S, Peen U, Dimoula M, Roed H, Ør Knudsen A, Staff S, Krog Vistisen A, Bjørge L, Mäenpää JU; AVANOVA investigators. Niraparib plus bevacizumab versus niraparib alone for platinum-sensitive recurrent ovarian cancer (NSGO-AVANOVA2/ENGOT-ov24): a randomised, phase 2, superiority trial. Lancet Oncol. 2019 Oct;20(10):1409-1419. doi: 10.1016/S1470-2045(19)30515-7. Epub 2019 Aug 29. PubMed PMID: 31474354.

9: Gray S, Khor XY, Yiannakis D. Niraparib as maintenance therapy in a patient with ovarian cancer and brain metastases. BMJ Case Rep. 2019 Aug 28;12(8). pii: e230738. doi: 10.1136/bcr-2019-230738. PubMed PMID: 31466953.

10: Zhang J, Zheng H, Gao Y, Lou G, Yin R, Ji D, Li W, Wang W, Xia B, Wang D, Hou J, Yan J, Hei Y, Zhang ZY, Milton A, Wu X. Phase I Pharmacokinetic Study of Niraparib in Chinese Patients with Epithelial Ovarian Cancer. Oncologist. 2019 Aug 22. pii: theoncologist.2019-0565. doi: 10.1634/theoncologist.2019-0565. [Epub ahead of print] PubMed PMID: 31439812.

11: Mirza MR, Bergmann TK, Mau-Sørensen M, Christensen RD, Åvall-Lundqvist E, Birrer MJ, Jørgensen M, Roed H, Malander S, Nielsen F, Lassen U, Brøsen K, Bjørge L, Mäenpää J. A phase I study of the PARP inhibitor niraparib in combination with bevacizumab in platinum-sensitive epithelial ovarian cancer: NSGO AVANOVA1/ENGOT-OV24. Cancer Chemother Pharmacol. 2019 Oct;84(4):791-798. doi: 10.1007/s00280-019-03917-z. Epub 2019 Aug 2. PubMed PMID: 31375879.

12: Konstantinopoulos PA, Waggoner S, Vidal GA, Mita M, Moroney JW, Holloway R, Van Le L, Sachdev JC, Chapman-Davis E, Colon-Otero G, Penson RT, Matulonis UA, Kim YB, Moore KN, Swisher EM, Färkkilä A, D'Andrea A, Stringer-Reasor E, Wang J, Buerstatte N, Arora S, Graham JR, Bobilev D, Dezube BJ, Munster P. Single-Arm Phases 1 and 2 Trial of Niraparib in Combination With Pembrolizumab in Patients With Recurrent Platinum-Resistant Ovarian Carcinoma. JAMA Oncol. 2019 Jun 13. doi: 10.1001/jamaoncol.2019.1048. [Epub ahead of print] PubMed PMID: 31194228; PubMed Central PMCID: PMC6567832.

13: Vinayak S, Tolaney SM, Schwartzberg L, Mita M, McCann G, Tan AR, Wahner-Hendrickson AE, Forero A, Anders C, Wulf GM, Dillon P, Lynce F, Zarwan C, Erban JK, Zhou Y, Buerstatte N, Graham JR, Arora S, Dezube BJ, Telli ML. Open-Label Clinical Trial of Niraparib Combined With Pembrolizumab for Treatment of Advanced or Metastatic Triple-Negative Breast Cancer. JAMA Oncol. 2019 Jun 13. doi: 10.1001/jamaoncol.2019.1029. [Epub ahead of print] PubMed PMID: 31194225; PubMed Central PMCID: PMC6567845.

14: Del Campo JM, Matulonis UA, Malander S, Provencher D, Mahner S, Follana P, Waters J, Berek JS, Woie K, Oza AM, Canzler U, Gil-Martin M, Lesoin A, Monk BJ, Lund B, Gilbert L, Wenham RM, Benigno B, Arora S, Hazard SJ, Mirza MR. Niraparib Maintenance Therapy in Patients With Recurrent Ovarian Cancer After a Partial Response to the Last Platinum-Based Chemotherapy in the ENGOT-OV16/NOVA Trial. J Clin Oncol. 2019 Nov 10;37(32):2968-2973. doi: 10.1200/JCO.18.02238. Epub 2019 Jun 7. PubMed PMID: 31173551; PubMed Central PMCID: PMC6839909.

15: Wallace K, Goble S, Isaacson J, Maloney L, Cameron T, Bedel J. Comment on: "Cost-Effectiveness of Niraparib Versus Routine Surveillance, Olaparib and Rucaparib for the Maintenance Treatment of Patients with Ovarian Cancer in the United States". Pharmacoeconomics. 2019 Aug;37(8):1065-1067. doi: 10.1007/s40273-019-00815-3. PubMed PMID: 31172449; PubMed Central PMCID: PMC6830408.

16: Guy H, Walder L, Fisher M. Response to 'Comment on "Cost-Effectiveness of Niraparib Versus Routine Surveillance, Olaparib and Rucaparib for the Maintenance Treatment of Patients with Ovarian Cancer in the United States"'. Pharmacoeconomics. 2019 Jul;37(7):965-967. doi: 10.1007/s40273-019-00803-7. PubMed PMID: 31044349.

17: McQueen RB, Whittington MD, Chapman RH, Kumar VM, Campbell JD. Comment on "Cost-Effectiveness of Niraparib Versus Routine Surveillance, Olaparib and Rucaparib for the Maintenance Treatment of Patients with Ovarian Cancer in the United States". Pharmacoeconomics. 2019 Jul;37(7):963-964. doi: 10.1007/s40273-019-00802-8. PubMed PMID: 31044348.

18: Moore KN, Secord AA, Geller MA, Miller DS, Cloven N, Fleming GF, Wahner Hendrickson AE, Azodi M, DiSilvestro P, Oza AM, Cristea M, Berek JS, Chan JK, Rimel BJ, Matei DE, Li Y, Sun K, Luptakova K, Matulonis UA, Monk BJ. Niraparib monotherapy for late-line treatment of ovarian cancer (QUADRA): a multicentre, open-label, single-arm, phase 2 trial. Lancet Oncol. 2019 May;20(5):636-648. doi: 10.1016/S1470-2045(19)30029-4. Epub 2019 Apr 1. Erratum in: Lancet Oncol. 2019 May;20(5):e242. PubMed PMID: 30948273.

19: Neeser K, O'Neil WM, Stern L, Harrow B, Travers K. Budget impact of niraparib as maintenance treatment in recurrent ovarian cancer following platinum-based chemotherapy. J Comp Eff Res. 2019 Jun;8(8):577-587. doi: 10.2217/cer-2018-0069. Epub 2019 Apr 2. PubMed PMID: 30935213.

20: Niraparib Shrinks BRCA-Mutated Prostate Tumors. Cancer Discov. 2019 Apr;9(4):OF7. doi: 10.1158/2159-8290.CD-NB2019-030. Epub 2019 Mar 1. PubMed PMID: 30824427.

Additional Information

Related CAS#
CAS#1038915-60-4 ( Niraparib free base);
CAS#1038915-64-8 ( Niraparib HCl salt);
CAS#1038915-73-9 ( Niraparib tosylate)

MK-4827 displays good pharmacokinetic properties and is currently in phase I clin. trials. This compd. displays excellent PARP 1 and 2 inhibition with IC50 = 3.8 and 2.1 nM, resp., and in a whole cell assay, it inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.  [See: Journal of Medicinal Chemistry (2009), 52(22), 7170-7185. ]
MK-4827 was found to be highly and similarly effective in both radiation schedules but maximum radiation enhancement was observed when MK-4827 was given at a dose of 50 mg/kg once daily (EF = 2.2). MK-4827 radiosensitized all four tumors studied regardless of their p53 status. MK-4827 reduced PAR levels in tumors by 1 h after administration which persisted for up to 24 h. This long period of PARP inhibition potentially adds to the flexibility of design of future clinical trials. Thus, MK-4827 shows high potential to improve the efficacy of radiotherapy. (source: Invest New Drugs. 2011 Nov 30. [Epub ahead of print])