Fluzoparib (SHR-3162)

Catalog No.S9712 Batch:S971201

Technical Data

Formula

C₂₂H₁₆F₄N₆O₂

Molecular Weight

472.40

CAS No.

1358715-18-0

Solubility (25°C)*

In vitro

DMSO

94 mg/mL (198.98 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 Corn oil	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity, with an IC50 of 1.46±0.72 nM for PARP1.

Targets

PARP ^[1]

In vitro

All four NSCLC cell lines (A549, H460, H1299, and PC9) shows decreased viability upon exposure to fluzoparib, and the effect is time and dose dependent. Fluzoparib acts synergistically to inhibit cell growth and promote apoptosis among lung cancer cells.^[2]

In vivo

An H460 cell xenograft mouse model is established to study the in vivo effects of fluzoparib and RT on tumor growth and survival. Treatment with RT + fluzoparib more effectively delayed tumor growth than treatment with either RT or fluzoparib individually. When combined with RT, fluzoparib conferres a significant survival benefit with no evidence of toxicity.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines human NSCLC cell lines A549, H460, H1299 and PC9 Concentrations 0–800 μM Incubation Time 24 h, 48 h, 72 h, 96 h Method Cells of all four NSCLC cell lines (A549, H460, H1299 and PC9) are plated in 96-well plates separately, with approximately 2 × 10³ cells added to each well. The cells are exposed to fluzoparib at different concentration (0–800 μM) in completed medium for 24, 48, 72, or 96 h. After exposure of the cells to fluzoparib for the indicated time period, the CellTiter 96 Aqueous Non-radioactive Cell Proliferation assay is used to detect cell viability, and IC50 values are calculated. The experiment is performed three times and mean and standard deviation (SD) values are calculated for further statistical analysis of the results.
Animal Study:^{^[2]}	Animal Models 5-6 week-old female Nu/Nu mice Dosages 1 mg/kg Administration IG

Cell Assay:^{^[2]}

Cell lines
human NSCLC cell lines A549, H460, H1299 and PC9
Concentrations
0–800 μM
Incubation Time
24 h, 48 h, 72 h, 96 h
Method
Cells of all four NSCLC cell lines (A549, H460, H1299 and PC9) are plated in 96-well plates separately, with approximately 2 × 10³ cells added to each well. The cells are exposed to fluzoparib at different concentration (0–800 μM) in completed medium for 24, 48, 72, or 96 h. After exposure of the cells to fluzoparib for the indicated time period, the CellTiter 96 Aqueous Non-radioactive Cell Proliferation assay is used to detect cell viability, and IC50 values are calculated. The experiment is performed three times and mean and standard deviation (SD) values are calculated for further statistical analysis of the results.

Animal Study:^{^[2]}

Animal Models
5-6 week-old female Nu/Nu mice
Dosages
1 mg/kg
Administration
IG

References

Selleck's Fluzoparib (SHR-3162) has been cited by 1 publication

Slow Dissociation from the PARP1-HPF1 Complex Drives Inhibitor Potency [ Biochemistry, 2023, 62(16):2382-2390]	PubMed: 37531469

Slow Dissociation from the PARP1-HPF1 Complex Drives Inhibitor Potency [ Biochemistry, 2023, 62(16):2382-2390]

PubMed: 37531469

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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