Umbralisib R-enantiomer (TGR-1202 R-enantiomer) 是 PI3Kδ 抑制剂,是 TGR-1202 活性较低的对映体。
CAS:1532533-69-9
分子式:C31H24F3N5O3
分子量:571.55
纯度:98%
存储:Store at -20°C
Background:
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
PI3Kδ
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) (Formula A) exhibits a 50% inhibitory concentration (IC50) with respect to the δ type PI3-kinase that is at least 20-fold lower than the inhibitor’s IC50 with respect to the rest of the other PI3K isoforms (i.e., a, β, and γ)[1].
[1]. Michael Weiss, et al. Combination of anti-cd20 antibody and pi3 kinase selective inhibitor. WO2014071125A1.