Fluzoparib
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MedKoo CAT#: 527603

CAS#: 1358715-18-0

Description: Fluzoparib, also known as SHR3162, is a poly (ADP-ribose) polymerase inhibitor (PARP) inhibitor potentially for the treatment of solid tumours.

Chemical Structure

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Fluzoparib
CAS# 1358715-18-0
Instruction

Theoretical Analysis

MedKoo Cat#: 527603
Name: Fluzoparib
CAS#: 1358715-18-0
Chemical Formula: C22H16F4N6O2
Exact Mass: 472.13
Molecular Weight: 472.404
Elemental Analysis: C, 55.94; H, 3.41; F, 16.09; N, 17.79; O, 6.77

Price and Availability

Size Price Availability Quantity
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
200mg USD 2950 2 Weeks
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Synonym: Fuzuloparib; SHR3162; SHR-3162; SHR 3162; Fluzoparib;

IUPAC/Chemical Name: 4-(4-fluoro-3-(2-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-a]pyrazine-7-carbonyl)benzyl)phthalazin-1(2H)-one

InChi Key: XJGXCBHXFWBOTN-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H16F4N6O2/c23-16-6-5-12(10-17-13-3-1-2-4-14(13)19(33)29-28-17)9-15(16)20(34)31-7-8-32-18(11-31)27-21(30-32)22(24,25)26/h1-6,9H,7-8,10-11H2,(H,29,33)

SMILES Code: O=C1NN=C(CC2=CC=C(F)C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)C5=C1C=CC=C5

Appearance: Solid powder

Purity: >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).

Solubility: Soluble in DMSO

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: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 472.40 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Li X, Yuan X, Wang Z, Li J, Liu Z, Wang Y, Wei L, Li Y, Wang X. Chidamide Reverses Fluzoparib Resistance in Triple-Negative Breast Cancer Cells. Front Oncol. 2022 Feb 18;12:819714. doi: 10.3389/fonc.2022.819714. PMID: 35251986; PMCID: PMC8894594.


2: Li N, Zhang Y, Wang J, Zhu J, Wang L, Wu X, Yao D, Wu Q, Liu J, Tang J, Yin R, Lou G, An R, Zhang G, Xia X, Li Q, Zhu Y, Zheng H, Yang X, Hu Y, Zhang X, Hao M, Huang Y, Lin Z, Wang D, Guo X, Yao S, Wan X, Zhou H, Yao L, Yang X, Cui H, Meng Y, Zhang S, Qu J, Zhang B, Zou J, Wu L. Fuzuloparib Maintenance Therapy in Patients With Platinum-Sensitive, Recurrent Ovarian Carcinoma (FZOCUS-2): A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase III Trial. J Clin Oncol. 2022 Aug 1;40(22):2436-2446. doi: 10.1200/JCO.21.01511. Epub 2022 Apr 11. PMID: 35404684.


3: Gong C, Wu J, Song W, Li H, Shi C, Gao Y, Shi Z, Li Z, Zhang M. Enhanced efficacy of combined fluzoparib and chidamide targeting in natural killer/T-cell lymphoma. Ann Hematol. 2023 Oct;102(10):2845-2855. doi: 10.1007/s00277-023-05359-3. Epub 2023 Jul 27. PMID: 37500898.


4: Wang L, Yang C, Xie C, Jiang J, Gao M, Fu L, Li Y, Bao X, Fu H, Lou L. Pharmacologic characterization of fluzoparib, a novel poly(ADP-ribose) polymerase inhibitor undergoing clinical trials. Cancer Sci. 2019 Mar;110(3):1064-1075. doi: 10.1111/cas.13947. Epub 2019 Feb 19. PMID: 30663191; PMCID: PMC6398880.


5: Luo J, Dai X, Hu H, Chen J, Zhao L, Yang C, Sun J, Zhang L, Wang Q, Xu S, Xu Y, Liu N, Ying G, Wang P. Fluzoparib increases radiation sensitivity of non- small cell lung cancer (NSCLC) cells without BRCA1/2 mutation, a novel PARP1 inhibitor undergoing clinical trials. J Cancer Res Clin Oncol. 2020 Mar;146(3):721-737. doi: 10.1007/s00432-019-03097-6. Epub 2019 Nov 30. PMID: 31786739.


6: Lee A. Fuzuloparib: First Approval. Drugs. 2021 Jul;81(10):1221-1226. doi: 10.1007/s40265-021-01541-x. Erratum in: Drugs. 2021 Jul 10;: Erratum in: Drugs. 2021 Sep;81(13):1597. PMID: 34118019; PMCID: PMC8380563.


7: Li D, Huang Z, Zhong J, Lin L, Zhang G, Zhuang W, Liu Z. Efficacy and safety of fluzoparib combined with anlotinib in extensive stage small cell lung cancer after first-line platinum-based chemotherapy: a multi-center, single-arm prospective phase II clinical study (STAMP study). BMC Cancer. 2023 Aug 14;23(1):753. doi: 10.1186/s12885-023-11230-5. PMID: 37580661; PMCID: PMC10424452.


8: Sun X, Chen W, Qu X, Chen Y. Case Report: Fluzoparib for multiple lines of chemotherapy refractory in metastatic cutaneous squamous cell carcinoma with BRCA2 pathogenic mutation. Front Pharmacol. 2022 Aug 12;13:968060. doi: 10.3389/fphar.2022.968060. PMID: 36034850; PMCID: PMC9411933.


9: Wu M, Li X, Sun J, Chen H, Ding Y. A phase I study of fluzoparib tablet formulation, an oral PARP inhibitor: effect of food on the pharmacokinetics and metabolism after oral dosing in healthy Chinese volunteers. Expert Opin Drug Metab Toxicol. 2021 Apr;17(4):503-508. doi: 10.1080/17425255.2021.1881480. Epub 2021 Feb 14. PMID: 33535835.


10: Luo L, Keyomarsi K. PARP inhibitors as single agents and in combination therapy: the most promising treatment strategies in clinical trials for BRCA- mutant ovarian and triple-negative breast cancers. Expert Opin Investig Drugs. 2022 Jun;31(6):607-631. doi: 10.1080/13543784.2022.2067527. Epub 2022 May 3. PMID: 35435784; PMCID: PMC9296104.


11: Fu J, Qiu F, Stolniceanu CR, Yu F, Zang S, Xiang Y, Huang Y, Matovic M, Stefanescu C, Tang Q, Wang F. Combined use of 177 Lu-DOTATATE peptide receptor radionuclide therapy and fluzoparib for treatment of well- differentiated neuroendocrine tumors: A preclinical study. J Neuroendocrinol. 2022 Apr;34(4):e13109. doi: 10.1111/jne.13109. Epub 2022 Mar 19. PMID: 35304807.


12: Li L, Xiang YX, Yang GP, Zhang XF, Yang XY, Yang S, Huang J. Pharmacokinetic effects of proton pump inhibitors on the novel PARP inhibitor fluzoparib: a single-arm, fixed-sequence trial in male healthy volunteers. Invest New Drugs. 2021 Jun;39(3):796-802. doi: 10.1007/s10637-020-01034-w. Epub 2021 Jan 9. PMID: 33420642.


13: Li N, Bu H, Liu J, Zhu J, Zhou Q, Wang L, Yin R, Wu X, Yao S, Gu K, Zhang H, Li G, Pan H, Wu Q, An R, Yang X, Zhu Y, Wan X, Duan W, Xiong J, Guo H, Lou G, Wang J, Hu W, Zhang X, Meng Y, Zhang B, Wang Y, Wang Q, Wu L. An Open-label, Multicenter, Single-arm, Phase II Study of Fluzoparib in Patients with Germline BRCA1/2 Mutation and Platinum-sensitive Recurrent Ovarian Cancer. Clin Cancer Res. 2021 May 1;27(9):2452-2458. doi: 10.1158/1078-0432.CCR-20-3546. Epub 2021 Feb 8. PMID: 33558426.


14: Li H, Liu R, Shao B, Ran R, Song G, Wang K, Shi Y, Liu J, Hu W, Chen F, Liu X, Zhang G, Zhao C, Jia R, Wang Q, Rugo HS, Zhang Y, Li G, Xu J. Phase I dose- escalation and expansion study of PARP inhibitor, fluzoparib (SHR3162), in patients with advanced solid tumors. Chin J Cancer Res. 2020 Jun;32(3):370-382. doi: 10.21147/j.issn.1000-9604.2020.03.08. PMID: 32694901; PMCID: PMC7369176.


15: Han Y, Chen MK, Wang HL, Hsu JL, Li CW, Chu YY, Liu CX, Nie L, Chan LC, Yam C, Wang SC, He GJ, Hortobagyi GN, Tan XD, Hung MC. Synergism of PARP inhibitor fluzoparib (HS10160) and MET inhibitor HS10241 in breast and ovarian cancer cells. Am J Cancer Res. 2019 Mar 1;9(3):608-618. PMID: 30949414; PMCID: PMC6448061.


16: Zhu L, Zhu C, Wang X, Liu H, Zhu Y, Sun X. The Combination of Icotinib Hydrochloride and Fluzoparib Enhances the Radiosensitivity of Biliary Tract Cancer Cells. Cancer Manag Res. 2020 Nov 19;12:11833-11844. doi: 10.2147/CMAR.S265327. PMID: 33239915; PMCID: PMC7682453.


17: Khan K, Jalal K, Uddin R. Pangenome diversification and resistance gene characterization in Salmonella Typhi prioritized RfaJ as a significant therapeutic marker. J Genet Eng Biotechnol. 2023 Nov 17;21(1):125. doi: 10.1186/s43141-023-00591-w. PMID: 37975995; PMCID: PMC10656401.


18: Stojanovic P, Luger K, Rudolph J. Slow Dissociation from the PARP1-HPF1 Complex Drives Inhibitor Potency. Biochemistry. 2023 Aug 15;62(16):2382-2390. doi: 10.1021/acs.biochem.3c00243. Epub 2023 Aug 2. PMID: 37531469; PMCID: PMC10433523.


19: Society of Obstetrics and Gynecology of Zhejiang Medical Association, Society of Urology of Zhejiang Medical Association, Committee of Breast Cancer of Zhejiang Anticancer Association, Committee of Clinical Pharmacy on Oncology of Zhejiang Anticancer Association (preparation), Committee of Urology of Zhejiang Society for Mathematical Medicine. Guidance on the management of adverse reactions induced by poly(ADP-ribose) polymerase inhibitors. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2022 Dec 25;51(6):765-774. English. doi: 10.3724/zdxbyxb-2022-0284. PMID: 36915979; PMCID: PMC10262009.


20: Chen X, Yang F, Zhao J, Tang Q, Heng J, Deng J, Zhang J, Chen Y, Li K, Wang J. Effect of fluconazole on the pharmacokinetics of fuzuloparib: an open-label, crossover study in Chinese healthy male volunteers. Cancer Chemother Pharmacol. 2022 Jan;89(1):141-148. doi: 10.1007/s00280-021-04376-1. Epub 2021 Dec 1. PMID: 34851444.