A-966492

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Chemical Information

Product name：A-966492	Purity：98% min
CAS NO：934162-61-5	Solubility：DMSO : ≥ 100 mg/mL (308.31 mM)
Molecular Formula：C₁₈H₁₇FN₄O	Package：Package according to customer requirements
Molecular Weight：324.352	Storage：Store at -20℃

Quality control

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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Afatinib dimaleate; Neratinib; Bosutinib; Bosutinib Intermediates; Bosutinib Monohydrate; Saracatinib; Dasatinib; NVP-BHG712; PP1; PP2; G007-LK; SU6656; Tirbanibulin; TPX-0005; Afatinib

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