A 966492 PARP Inhibitor Cas 934162-61-5
Chemical Information
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Product name:A-966492 |
Purity:98% min |
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CAS NO:934162-61-5 |
Solubility:DMSO : ≥ 100 mg/mL (308.31 mM) |
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Molecular Formula:C18H17FN4O |
Package:Package according to customer requirements |
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Molecular Weight:324.352 |
Storage:Store at -20℃ |
Remarks
A-966492 is a potent PARP inhibitor, which displayed excellent potency against the PARP-1 enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. It also demonstrated good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin.
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References
[1]. Penning TD, et al. Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious
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