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Chemical Structure| 1358715-18-0 Chemical Structure| 1358715-18-0

Structure of Fluzoparib
CAS No.: 1358715-18-0

Chemical Structure| 1358715-18-0

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Fluzoparib is an orally effective PARP1 inhibitor that selectively inhibits DNA repair mechanisms.

Synonyms: SHR3162; Fuzuloparib; HS10160

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Product Details of Fluzoparib

CAS No. :1358715-18-0
Formula : C22H16F4N6O2
M.W : 472.40
SMILES Code : O=C1NN=C(CC2=CC=C(F)C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)C5=C1C=CC=C5
Synonyms :
SHR3162; Fuzuloparib; HS10160
MDL No. :MFCD32899277

Safety of Fluzoparib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Fluzoparib

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 2.5 µM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
GBC-SD 5 μM 4 hours Inhibited cell proliferation and enhanced radiosensitivity Cancer Manag Res. 2020 Nov 19;12:11833-11844
OVCA433 5 µM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
DOV13 625 nM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
BT-549 625 nM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
HCCC-9810 10 μM 4 hours Inhibited cell proliferation and enhanced radiosensitivity Cancer Manag Res. 2020 Nov 19;12:11833-11844
MDA-MB-468-FR 80 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on drug-resistant MDA-MB-468-FR cells, results showed that the viability of drug-resistant cells was significantly higher than that of parental cells Front Oncol. 2022 Feb 18;12:819714
HCC1937-FR 60 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on drug-resistant HCC1937-FR cells, results showed that the viability of drug-resistant cells was significantly higher than that of parental cells Front Oncol. 2022 Feb 18;12:819714
MDA-MB-468 15 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on MDA-MB-468 cells, results showed that cell growth was significantly reduced with increasing Fluzoparib concentration Front Oncol. 2022 Feb 18;12:819714
HCC1937 6 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on HCC1937 cells, results showed that cell growth was significantly reduced with increasing Fluzoparib concentration Front Oncol. 2022 Feb 18;12:819714
NCI–H929B (H929B, bortezomib-resistant) 2.5, 5, 10 nM 24 hours To evaluate the effect of Fluzoparib on the viability and apoptosis of drug-resistant MM cells. Results showed that Fluzoparib significantly inhibited the proliferation of H929B cells and induced apoptosis. Biochem Biophys Rep. 2024 Jul 7;39:101781
NCI–H929 (H929) 2.5, 5, 10 nM 24 hours To evaluate the effect of Fluzoparib on the viability and apoptosis of MM cells. Results showed that Fluzoparib significantly inhibited the proliferation of H929 and H929B cells and induced apoptosis. Biochem Biophys Rep. 2024 Jul 7;39:101781

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice HCC1937-FR xenograft model Subcutaneous injection 25 mg/kg/bid (Fluzoparib), 5 mg/kg/bw (Chidamide) Twice daily for 21 days Evaluate the antitumor effects of Fluzoparib and Chidamide on HCC1937-FR xenograft model, results showed that the combination significantly inhibited tumor growth Front Oncol. 2022 Feb 18;12:819714
BALB/c nude mice Subcutaneous MM tumor model Oral 30 mg/kg Once daily for 13 days To evaluate the inhibitory effect of Fluzoparib on MM tumor growth in vivo. Results showed that Fluzoparib significantly suppressed tumor volumes and weights and promoted apoptosis of tumor tissue. Biochem Biophys Rep. 2024 Jul 7;39:101781

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04333134 Healthy Volunteers PHASE1 COMPLETED 2020-06-30 Atridia Pty Limited, Sydney, N... More >>ew South Wales, 2000, Australia Less <<
NCT03509636 Ovarian Cancer PHASE1 COMPLETED 2020-07-23 Cancer Hospital Chinese Academ... More >>y of Medical Sciences, Beijing, Beijing, China Less <<
NCT03062982 Solid Tumor PHASE1 COMPLETED 2017-01-04 the First Hosital of Jilin Uni... More >>versity, Changchun, Jilin, China Less <<
NCT04425876 Pancreatic Cancer PHASE1 UNKNOWN 2023-09-01 Ruijin Hospital, Shanghai Jiao... More >>tong University School of Medicine, Shanghai, Shanghai, China Less <<
NCT02575651 Advanced Solid Malignancies PHASE1 COMPLETED 2025-06-18 No.307 Hospital, Academy of Mi... More >>litary Medical Sciences, Beijing, Beijing, 100039, China|Beijing Cancer Hospital, Beijing, Beijing, 100142, China Less <<
NCT04341077 Healthy Adult Male and Female ... More >>Volunteers Less << PHASE1 UNKNOWN 2020-10-20 -
NCT02759666 Neoplasm|Solid Tumors PHASE1 COMPLETED 2019-04-26 Border Medical Oncology, Albur... More >>y, New South Wales, 2640, Australia|Liverpool Hospital, Liverpool, New South Wales, 2170, Australia|Linear, Melbourne, Australia Less <<
NCT04535687 Renal Cell Carcinoma PHASE2 COMPLETED 2023-06-12 The Affiliated Nanjing Drum To... More >>wer Hospital of Nanjing University Medical School, Nanjing, Jiangsu, 210000, China Less <<
NCT06541314 Ovarian Cancer PHASE2 RECRUITING 2026-05-31 Qilu Hospital of Shandong Univ... More >>ersity, Jinan, Shandong, 250000, China Less <<
NCT05440006 Solid Tumor PHASE1 COMPLETED 2022-07-20 Wannan Medical College Yijisha... More >>n Hospital, Wuhu, Anhui, 241000, China Less <<
NCT04694365 Hepatic Impairment|Healthy Sub... More >>jects Less << PHASE1 COMPLETED 2024-06-19 Henan Infectious Diseases Hosp... More >>ital, Zhengzhou, Henan, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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