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E7449

🥰Excellent
Catalog No. T4471Cas No. 1140964-99-3
Alias UNII-9X5A2QIA7C, Stenoparib

E7449 (UNII-9X5A2QIA7C) 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.

E7449

E7449

🥰Excellent
Purity: 97.13%
Catalog No. T4471Alias UNII-9X5A2QIA7C, StenoparibCas No. 1140964-99-3
E7449 (UNII-9X5A2QIA7C) 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.
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$85In Stock
10 mg$123In Stock
25 mg$198In Stock
50 mg$298In Stock
100 mg$443In Stock
200 mg$655In Stock
1 mL x 10 mM (in DMSO)$95In Stock
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Purity:97.13%
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Product Introduction

Bioactivity
Description
E7449 (UNII-9X5A2QIA7C) 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.
Targets&IC50
TNKS2:50 nM (IC50), PARP1:2 nM (IC50), TNKS1:50 nM (IC50), PARP2:1 nM (IC50)
In vitro
E7449 shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. E7449 traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). E7449 most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). E7449 (10 μM) inhibits Wnt signaling in SW480 cells[1].
In vivo
E7449 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[1].
AliasUNII-9X5A2QIA7C, Stenoparib
Chemical Properties
Molecular Weight317.34
FormulaC18H15N5O
Cas No.1140964-99-3
SmilesO=c1[nH][nH]c2nc(CN3Cc4ccccc4C3)nc3cccc1c23
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 6.4 mg/mL (20.17 mM), Sonication and heating are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.1512 mL15.7560 mL31.5119 mL157.5597 mL
5 mM0.6302 mL3.1512 mL6.3024 mL31.5119 mL
10 mM0.3151 mL1.5756 mL3.1512 mL15.7560 mL
20 mM0.1576 mL0.7878 mL1.5756 mL7.8780 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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