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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
2 mg | $54 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $122 | In Stock | |
25 mg | $247 | In Stock | |
50 mg | $372 | In Stock | |
100 mg | $578 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
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 | PARP2:1 nM (IC50), TNKS2:50 nM (IC50), PARP1:2 nM (IC50), TNKS1:50 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]. |
Alias | Stenoparib, UNII-9X5A2QIA7C |
Molecular Weight | 317.34 |
Formula | C18H15N5O |
Cas No. | 1140964-99-3 |
Storage | Powder: -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
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