2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Fluzoparib

Fluzoparib  (Synonyms: SHR3162; Fuzuloparib)

Cat. No.: HY-114778 Purity: 99.85%
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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.

For research use only. We do not sell to patients.

Fluzoparib Chemical Structure

Fluzoparib Chemical Structure

CAS No. : 1358715-18-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 182 In-stock
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5 mg USD 165 In-stock
10 mg USD 275 In-stock
25 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Fluzoparib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Fluzoparib

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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  • Customer Review

Description

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[1].

IC50 & Target[1]

PARP-1

1.46±0.72  nM (IC50)

In Vitro

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.

Fluzoparib Related Antibodies
In Vivo

Fluzoparib (oral gavage; 0.3, 1, or 3 mg/kg; single dose) exhibits a good pharmacokinetic profile in Female Balb/cA nude mice (5-6 weeks old) mice bearing MDA-MB-436. After a single oral dose, fluzoparib is rapidly absorbed and rapidly cleared from blood at all dose levels; plasma concentrations of fluzoparib quickly reaches maximum within 2 hours. In contrast, concentrations of fluzoparib in tumor remains at high levels even at 24 hours after dosing (57.9 ng/g , 39.3 ng/g, and 85.6 ng/g for doses of 0.3, 1, and 3 mg/kg, respectively)[1].
Fluzoparib (oral gavage; 30 mg/kg; 21 days) apparently inhibits the growth of tumor with an inhibition rate of 59% (day 21) at 30 mg/kg, and it does not cause significant loss of body weight in Nude mice bearing MDA-MB-436 (BRCA1-deficient) model[1].
Fluzoparib (3mg/kg) combines with Cisplatin, Paclitaxel, or Apatinib (oral gavage; BID; 21 days) causes growth inhibition with rates of 61.4%, 55.3%, and 72.8%, respectively.
Fluzoparib, Cisplatin, and Apatinib combination or Fluzoparib, Paclitaxel, and Apatinib combination can cause growth inhibition with rates of 84.9% and 75.6% (day 21), respectively in vivo.
The 2-drug combination of Fluzoparib with cisplatin and The 3-drug Fluzoparib, Cisplatin, and Apatinib combination lead to loss of body weight, whereas no apparent toxicity was observed in other combinations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

472.40

Formula

C22H16F4N6O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1169 mL 10.5843 mL 21.1685 mL
5 mM 0.4234 mL 2.1169 mL 4.2337 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.85%

COA (248 KB) HNMR (290 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

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
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Fluzoparib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fluzoparib1358715-18-0SHR3162 FuzuloparibSHR 3162SHR-3162PARPpoly ADP ribose polymerasehomologous recombination repairPARP1ovariancancerInhibitorinhibitorinhibit

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