1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. Stenoparib

Stenoparib  (Synonyms: E7449; 2X-121)

Cat. No.: HY-12418 Purity: ≥98.0%
COA Handling Instructions

Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

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

Stenoparib Chemical Structure

Stenoparib Chemical Structure

CAS No. : 1140964-99-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Stenoparib

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

IC50 & Target[1]

PARP2

1 nM (IC50)

PARP1

2 nM (IC50)

TNKS1

50 nM (IC50)

TNKS2

50 nM (IC50)

In Vitro

Stenoparib is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate. Stenoparib shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. Stenoparib traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). Stenoparib most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). Stenoparib (10 μM) inhibits Wnt signaling in SW480 cells[1].

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

In Vivo

Stenoparib moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model. Stenoparib (30 or 100 mg/kg, p.o.) inhibits PARP, shows anti-tumor activity, and is well-tolerated without any obvious body weight loss or deaths in a BRCA mutant xenograft model. Stenoparib (30, 100 or 300 mg/kg, p.o.) suppresses re-growth of hair in a dose dependent manner, and blocks Wnt signaling in C57BL/6 mice. Stenoparib (100 mg/kg, p.o.) combined with MEK inhibitor exhibits antitumor activity in a Wnt1 subcutaneous model (mammary tumors initially isolated from Wnt1 (int-1) transgenic mice)[1].

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

Clinical Trial
Molecular Weight

317.34

Formula

C18H15N5O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NNC2=C3C1=CC=CC3=NC(CN4CC5=C(C=CC=C5)C4)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (20.17 mM; Need ultrasonic and warming; 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 3.1512 mL 15.7560 mL 31.5119 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

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

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

References
Kinase Assay
[1]

Briefly, 24 to 48 h after transfection, cells are washed 3× in ice-cold PBS and lysed for 20 min on ice in cell lysis buffer (CLB: 50 mM HEPES, pH 7.4, 150 mM NaCl, 1 mM MgCl2, 1 mM EGTA, 1 mM DTT, 1% TritonX-100, 1 μg/mL leupeptin, aprotinin, pepstatin, PMSF). Lysates are subject to ultracentrifugation at 100,000 g for 30 min. Cleared lysates are incubated for 1 h at 4°C with anti-GFP antibody (3E6) and pre-bound protein A magnetic beads. Beads are then washed 1 × 5 min in CLB, followed by 3 × 10 min washes in CLB containing 1 M NaCl, and 1 × 5 min wash in PARP reaction buffer (PRB; 50 mM Tris, pH 7.5, 50 mM NaCl, 0.5 mM DTT, 0.1% TritonX-100, 1 μg/mL leupeptin, aprotinin, pepstatin). NAD+ incorporation reactions are performed in PRB containing 10 μM NAD+ supplemented with 32P-NAD+ at 1:20 ratio for 30 min at 25°C. For PARPs with low incorporation signals (PARP4, 5a and 16), NAD+ incorporation is performed at 1:5 ratio for 1 h at 25°C. Beads are then re-suspended in Laemmli sample buffer, heated to 65°C for 10 min, the beads removed using a magnet, and the supernatant spotted onto Whatman paper. Samples are analyzed via phosphorimaging[1].

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

Cell Assay
[1]

Proliferation assays are performed in a panel of 32 isogenic DT40 cell lines, in which each line is deficient in a distinct DNA repair gene. Cells are seeded and incubated with test compound at various concentrations for 2-3 days (∼ 8 cell cycles). Cell growth is assessed using XTT and IC50 values are calculated using the GraphPad Prism 5 software version 5.02. Each experiment is conducted in duplicate and a minimum of 3 separate experiments are performed. Human breast cancer cell lines, HCC1143, HCC70, HCC1806, MDA-MB-436, T47D, MDA-MB-157, MDA-MB-231, MDA-MB-468, MDA-MB-453, BT-20 and Hs578T are used. For cell line panel assays, cells are maintained and assayed in RPMI 1640 or DMEM medium containing 10% FBS. For proliferation assays cells are plated at low density in 96 well plates. Stenoparib is added at various concentrations and plates incubated for a total of 8 days; compound and medium are replenished on day 4. Cell growth is assessed using the CellTiter-Glo cell viability assay. Each experiment is conducted in duplicate and a minimum of 3 separate experiments are performed[1].

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

Animal Administration
[1]

Temozolomide (TMZ) combination in B16-F10 isograft model: female C57BL/6 mice are inoculated subcutaneously with B16-F10 cells (2 × 105). Following randomization by body weight, drug treatment is initiated 1 day post-inoculation. Both Stenoparib and TMZ are formulated in 0.5% methyl cellulose and orally administrated once per day. TMZ is administered daily on days 1 to 5 at 50 mg/kg as a single agent or in combination. Stenoparib is administered daily on days 1 to 7 at doses of 10, 30 and 100 mg/kg in combination with TMZ and at a dose of 100 mg/kg as a single agent. The control group is treated with vehicle (0.5% methyl cellulose in water). Stenoparib or vehicle is administered first and when dosing of all animals is complete TMZ is administered to animals receiving the combination[1].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1512 mL 15.7560 mL 31.5119 mL 78.7799 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 mL 15.7560 mL
10 mM 0.3151 mL 1.5756 mL 3.1512 mL 7.8780 mL
15 mM 0.2101 mL 1.0504 mL 2.1008 mL 5.2520 mL
20 mM 0.1576 mL 0.7878 mL 1.5756 mL 3.9390 mL
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Stenoparib 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.

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