1. Cell Cycle/DNA Damage Apoptosis
  2. Apoptosis Poly(ADP-ribose) Glycohydrolase (PARG)
  3. PARG-IN-4

PARG-IN-4 (Formula (A)) is an orally available PARG inhibitor (EC50=1.9 nM) with cell membrane permeability. PARG-IN-4 can effectively inhibit tumor growth in mouse models. PARG-IN-4 can be used in cancer research.

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PARG-IN-4

PARG-IN-4 構造式

CAS 番号 : 2988890-20-4

容量 価格(税別) 在庫状況 数量
1 mg $260 在庫あり
5 mg $650 在庫あり
10 mg $1050 在庫あり
25 mg $2100 在庫あり
50 mg $3400 在庫あり
100 mg $5450 在庫あり
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500 mg   お問い合わせ  

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製品説明

PARG-IN-4 (Formula (A)) is an orally available PARG inhibitor (EC50=1.9 nM) with cell membrane permeability. PARG-IN-4 can effectively inhibit tumor growth in mouse models. PARG-IN-4 can be used in cancer research[1].

IC50 & Target

EC50: 1.9 nM (Poly(ADP-ribose) Glycohydrolase (PARG))

体外実験

PARG-IN-4 (Formula (A)) affects the cell viability of SNU601 and RMUGS cells with EC50 of 11 nM and 4.2 nM, respectively; and exhibits antiproliferative activity against ovarian and breast cancer cells[1].

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

Cell Proliferation Assay[1]

Cell Line: Ovarian cancer cells: RMUG-S, Kuramochi, OBISE, OVMANA; Breast cancer cells: HCC1569, CAL851, HCC1937, HCC1954S
Concentration: IC50
Incubation Time:
Result: Exhibited anti-proliferative activity against ovarian cancer cells and breast cancer cells with IC50s of 8 nM (RMUG-S), 9 nM (Kuramochi), 50 nM (OVISE), 120 nM (OVMANA); 0.08 μM (HCC1569), 0.1 μM (CAL851), 0.22 μM (HCC1937), 0.37 μM (HCC1954), respectively.
体内実験

PARG-IN-4 (Formula (A)) (100 mg/kg; po; QD; 45 d) induces tumor regression in a patient-derived HBCx-34 xenograft mouse model[1].

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

Animal Model: HBCx-34 Patient-derivedxenograft(PDX) Mouse Model: Female Athymic Nude-Foxnlnu mice[1]
Dosage: 100 mg/kg, 10 mL/kg
Administration: po; QD×45
Result: Resulted tumor growth inhibition with TGI rate of 110%.
分子量

497.59

分子式

C20H25F2N7O2S2

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1(CC1)NS(=O)(C2=CC(N3C[C@@H](N[C@H](C3)C)C)=C(C=NN4C5=NN=C(C(F)F)S5)C4=C2)=O

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
溶剤 & 溶解度
体外: 

DMSO : 20 mg/mL (40.19 mM; ultrasonic and warming and heat to 80°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 2.0097 mL 10.0484 mL 20.0969 mL
5 mM 0.4019 mL 2.0097 mL 4.0194 mL
10 mM 0.2010 mL 1.0048 mL 2.0097 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

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体積 (終了)

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体内:

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 mg/mL (4.02 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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% (20% SBE-β-CD in Saline)

    Solubility: 2 mg/mL (4.02 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
参考文献

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 2.0097 mL 10.0484 mL 20.0969 mL 50.2422 mL
5 mM 0.4019 mL 2.0097 mL 4.0194 mL 10.0484 mL
10 mM 0.2010 mL 1.0048 mL 2.0097 mL 5.0242 mL
15 mM 0.1340 mL 0.6699 mL 1.3398 mL 3.3495 mL
20 mM 0.1005 mL 0.5024 mL 1.0048 mL 2.5121 mL
25 mM 0.0804 mL 0.4019 mL 0.8039 mL 2.0097 mL
30 mM 0.0670 mL 0.3349 mL 0.6699 mL 1.6747 mL
40 mM 0.0502 mL 0.2512 mL 0.5024 mL 1.2561 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
PARG-IN-4
製品番号:
HY-156881
数量:
MCE 日本正規代理店: