Duvelisib，[IPI-145, INK1197]；≥99% (HPLC)

General description

一种选择性强且具有潜在免疫调节和抗肿瘤活性的PI3K δ/γ抑制剂,Ki和IC50分别为23pM/243pM和1nM/50nM。

Duvelisib is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, PI3K delta/gamma inhibitor IPI 145 prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases。

Duvelisib是磷酸肌醇3激酶（PI3K）的δ和γ亚型的口服生物利用型，高选择性和有效小分子抑制剂，具有潜在的免疫调节和抗肿瘤活性。 给药后，PI3Kδ/γ抑制剂IPI 145阻止了PI3Kδ/γ介导的信号通路的激活，这可能导致表达PI3Kδ/γ的肿瘤细胞中细胞增殖的减少。 与其他PI3K亚型不同，δ和γ亚型主要在血液系统恶性肿瘤，炎性和自身免疫性疾病中过表达。

Properties

安全信息