Fluzoparib
Based on 4 publication(s) in Google Scholar
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.96%
- CAS 番号: 1358715-18-0
- 分子式: C22H16F4N6O2
- 分子量:472.40
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
NMPA-Approved Drug Library
HY-L053
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Radiosensitizer Library
HY-L179
-
Bioactive Compound Library Max
HY-L181
-
Epigenetics Compound Library Mini
HY-L005M
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Cancer Approved Drug Library
HY-L213
MedChemExpress（MCE）の使用を引用している文献 Fluzoparib
More
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Cell Migration/Invasion Assay
-
Flow Cytometry
-
IF
-
Histological Imaging/Staining
生物活性
|
PARP-1 1.46±0.72 nM (IC50) |
Fluzoparib (30 μM; 24 hour) increases the levels of γH2AX in a concentration-dependent manner in both BRCA2-deficient V-C8 cells and BRCA1-deficient MDA-MB-436 cells, but not in BRCA-proficient V-C8#13-5 cells[1]. Fluzoparib (10 μM; 24 hour) increases levels of both pCDK1 and cyclin B, indicating activation of the G2/M checkpoint in MDA-MB-436 cells[1].Fluzoparib (10 μM; 72 hour) increases the processing of caspase-3, -8, and -9 concentration-dependently, it induces G2/M arrest and apoptosis in HR-deficient MDA-MB-436 cells cells[1].Fluzoparib is preferentially efficacious against HR-deficient cells, such as BRCA1-deficient (UWB1.289), MDA-MB-436, BRCA2-deficient (V-C8), BRCA1-deficientBRCA2-mutated (MX-1) and BRCA1 hypermethylated (OVCAR-8) cells with IC50 values of 0.51 μM, 1.57 μM, 0.053 μM, 1.57 μM, and 1.43 μM, respectively. The IC50 values for HR-proficient cells (V-C8#13-5 and UWB1.289 BRCA1) are both >10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1358715-18-0
-
性状 Solid
-
分子量 472.40
-
分子式 C22H16F4N6O2
-
Color White to off-white
-
SMILES
O=C1NN=C(CC2=CC=C(F)C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)C5=C1C=CC=C5
-
別名
SHR3162; Fuzuloparib
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Targeting de novo pyrimidine synthesis confers vulnerability to copper-mediated ATR inactivation in PARP inhibitor-resistant ovarian cancer. [Abstract]2026 Feb 25;17(1):3142. PMID: 41735312 -
Acta Pharmacol Sin
Hepatitis B virus core protein promotes liver cancer progression by stabilizing CANX and suppressing IRF7 transcription. [Abstract]2025 Jun 13. PMID: 40514420 -
Int Immunopharmacol
Fluzoparib disrupts Golgi apparatus to inhibit O-GlcNAcylation and nuclear translocation of β-catenin to attenuate ovarian cancer invasion and metastasis. [Abstract]2025 Sep 23:162:115158. PMID: 40602265
Fluzoparib purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115158. [Abstract]
Cells were treated with 0, 5, 10, 20, 40, and 60 μM FZ (Fluzoparib) for 24 hours, and cell viability was subsequently assessed using the CCK-8 assay.
Fluzoparib purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115158. [Abstract]
The effect of 24-hour treatment with 0, 20, 40, and 60 μM FZ (Fluzoparib) on the migration ability of A2780 and SKOV3 cells was assessed using a scratch assay.
Fluzoparib purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115158. [Abstract]
A2780 and SKOV3 cells were treated with FZ (Fluzoparib) at concentrations of 0, 20, 40, and 60 μM for 24 h, and apoptosis was assessed using flow cytometry.
Fluzoparib purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115158. [Abstract]
FZ (Fluzoparib: 40 μM). Immunofluorescence was used to further assess the expression levels of β-catenin.
Fluzoparib purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115158. [Abstract]
FZ (Fluzoparib: 30 mg/kg). H&E staining of vital organs.
-
Molecules
2022 Sep 21;27(19):6219. PMID: 36234755
溶剤 & 溶解度
DMSO : 33.33 mg/mL (70.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Lei Wang, et al. Pharmacologic characterization of fluzoparib, a novel poly(ADP-ribose) polymerase inhibitor undergoing clinical trials. Cancer Sci. 2019 Mar;110(3):1064-1075. [Content Brief]
[2]. Huiping Li, et al. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1169 mL | 10.5843 mL | 21.1685 mL | 52.9213 mL |
| 5 mM | 0.4234 mL | 2.1169 mL | 4.2337 mL | 10.5843 mL | |
| 10 mM | 0.2117 mL | 1.0584 mL | 2.1169 mL | 5.2921 mL | |
| 15 mM | 0.1411 mL | 0.7056 mL | 1.4112 mL | 3.5281 mL | |
| 20 mM | 0.1058 mL | 0.5292 mL | 1.0584 mL | 2.6461 mL | |
| 25 mM | 0.0847 mL | 0.4234 mL | 0.8467 mL | 2.1169 mL | |
| 30 mM | 0.0706 mL | 0.3528 mL | 0.7056 mL | 1.7640 mL | |
| 40 mM | 0.0529 mL | 0.2646 mL | 0.5292 mL | 1.3230 mL | |
| 50 mM | 0.0423 mL | 0.2117 mL | 0.4234 mL | 1.0584 mL | |
| 60 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8820 mL |
Fluzoparib 関連分類
HY-114778 関連分類
Powered by Bioz