2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease
  3. PARP Cytochrome P450
  4. PARP7-IN-15

PARP7-IN-15 is an orally active and selective PARP7 inhibitor with an IC50 of 0.56 nM. PARP7-IN-15 inhibits the enzymatic activity of PARP7 and induces anti-tumor activity against lung cancer in vivo. PARP7-IN-15 can be used for the research of lung cancer.

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PARP7-IN-15

PARP7-IN-15 構造式

CAS 番号 : 2819998-97-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 866 在庫あり
Solution
10 mM * 1 mL in DMSO USD 866 在庫あり
Solid
5 mg $700 在庫あり
10 mg $1125 在庫あり
25 mg $2250 在庫あり
50 mg $3600 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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PARP7-IN-15 関連抗体

Top Publications Citing Use of Products

PARP アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Cytochrome P450 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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製品説明

PARP7-IN-15 is an orally active and selective PARP7 inhibitor with an IC50 of 0.56 nM. PARP7-IN-15 inhibits the enzymatic activity of PARP7 and induces anti-tumor activity against lung cancer in vivo. PARP7-IN-15 can be used for the research of lung cancer[1].

IC50 & Target

PARP7

0.56 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-436 IC50
> 10 μM
Compound: 18
Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 7 days by luminescence based assay
Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 7 days by luminescence based assay
[PMID: 37826932]
NCI-H1373 IC50
4.1 nM
Compound: 18
Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay
Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay
[PMID: 37826932]
体外実験

PARP7-IN-15 (compound 18) (4 days) potently inhibits the proliferation of PARP7-sensitive NCI-H1373 human lung cancer cells, with an IC50 of 4.1 nM[1].
PARP7-IN-15 (0.1 μM; 7 days) exhibits only extremely low antiproliferative activity against PARP7-insensitive human breast cancer MDA-MB-436 cells, with an IC50 >10 μM[1].
PARP7-IN-15 (24 h) significantly stimulates the expression of IFN-β in RAW246.7 mouse macrophages[1].
PARP7-IN-15 inhibits human CYP2C9 (IC50 = 2.01 μM) and CYP2C19 (IC50 = 7.55 μM) enzymes, but shows no significant inhibitory effect on CYP1A2, CYP2D6 or CYP3A4 (IC50 >30 μM)[1].

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

PARP7-IN-15 関連抗体

Cell Proliferation Assay[1]

Cell Line: PARP7-insensitive MDA-MB-436 human breast cancer cells
Concentration: 0.1 μM
Incubation Time: 7 days
Result: Showed no obvious inhibition of MDA-MB-436 cell proliferation at 0.1 μM.
Had an IC50 value for proliferation inhibition of >10 μM, indicating very high selectivity for PARP7-sensitive cells.
Parmacokinetics
Species Dose Route Tmax T1/2 Cmax AUC Bioavailability CL Vss
Mice[1] 2 mg/kg i.v. / 0.7 h / 680 ng·h/mL / 49.2 mL/min/kg 1770 mL/kg
Mice[1] 10 mg/kg p.o. 0.4 h 3.7 h 752 μg/mL 1146 ng·h/mL 33.9 % / /
体内実験

PARP7-IN-15 (30 mg/kg; p.o.; once daily; for 21 consecutive days) exhibits potent in vivo anti-tumor activity in the NCI-H1373 lung cancer xenograft mouse model[1].

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

Animal Model: CB17 SCID mice treated NCI-H1373 tumors (female, 6-8 weeks old)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 75.2%.
Caused no animal death or significant body weight loss during the treatment period.
分子量

562.46

分子式

C23H24F6N6O4
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C(F)(F)F)=C(N2CC[C@H]2COCCC(N3C[C@@H](COC4=C5N=CC(C(F)(F)F)=C4)N5CC3)=O)C=NN1
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 : 200 mg/mL (355.58 mM; Need ultrasonic; 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 1.7779 mL 8.8895 mL 17.7790 mL
5 mM 0.3556 mL 1.7779 mL 3.5558 mL
10 mM 0.1778 mL 0.8890 mL 1.7779 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

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

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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）

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体積 （開始）

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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: ≥ 5 mg/mL (8.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (8.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 1.7779 mL 8.8895 mL 17.7790 mL 44.4476 mL
5 mM 0.3556 mL 1.7779 mL 3.5558 mL 8.8895 mL
10 mM 0.1778 mL 0.8890 mL 1.7779 mL 4.4448 mL
15 mM 0.1185 mL 0.5926 mL 1.1853 mL 2.9632 mL
20 mM 0.0889 mL 0.4445 mL 0.8890 mL 2.2224 mL
25 mM 0.0711 mL 0.3556 mL 0.7112 mL 1.7779 mL
30 mM 0.0593 mL 0.2963 mL 0.5926 mL 1.4816 mL
40 mM 0.0444 mL 0.2222 mL 0.4445 mL 1.1112 mL
50 mM 0.0356 mL 0.1778 mL 0.3556 mL 0.8890 mL
60 mM 0.0296 mL 0.1482 mL 0.2963 mL 0.7408 mL
80 mM 0.0222 mL 0.1111 mL 0.2222 mL 0.5556 mL
100 mM 0.0178 mL 0.0889 mL 0.1778 mL 0.4445 mL
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PARP7-IN-15 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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

質量   濃度   体積   分子量 *
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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.

Keywords:

PARP7-IN-152819998-97-3PARPCytochrome P450poly ADP ribose polymerase CYPsRAW246.7 mouse macrophagesBeagle dogsPARP7lung cancerNCI-H1373 human lung cancer cellsCYP2C9ICR miceCYP2C19MDCKII-MDR1 cell monolayersMDA-MB-436 human breast cancer cellsInhibitorinhibitorinhibit

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