Stenoparib
Based on 2 publication(s) in Google Scholar
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.
- Purity : 98.0%
- CAS No.: 1140964-99-3
- Formula: C18H15N5O
- Molecular Weight:317.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Stenoparib
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Biological Activity
Description
IC50 & Target
[1]|
PARP2 1 nM (IC50) |
PARP1 2 nM (IC50) |
TNKS1 50 nM (IC50) |
TNKS2 50 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AML12 | CC50 |
1.39 μM
Compound: E7449
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Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 7 days by MTT assay
Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 7 days by MTT assay
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[PMID: 35504210] |
| HCT-116 | IC50 |
6.71 μM
Compound: E7449
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
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[PMID: 35504210] |
| MDA-MB-231 | IC50 |
2.89 μM
Compound: E7449
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
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[PMID: 35504210] |
| MDA-MB-468 | IC50 |
4.17 μM
Compound: E7449
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay
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[PMID: 35504210] |
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1140964-99-3
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Appearance Solid
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Molecular Weight 317.34
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Formula C18H15N5O
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Color Light yellow to yellow
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SMILES
O=C1NNC2=C3C1=CC=CC3=NC(CN4CC5=C(C=CC=C5)C4)=N2
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Synonyms
E7449; 2X-121
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (701 KB)
- English - EN (701 KB)
- Français - FR (701 KB)
- Deutsch - DE (701 KB)
- Norwegian - NO (701 KB)
- Español - ES (701 KB)
- Swedish - SV (701 KB)
- Italian - IT (701 KB)
- Korean - KR (701 KB)
- Portuguese - PT (701 KB)
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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, 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 |
Stenoparib Related Classifications
HY-12418 Related Classifications
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