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
| Iupac Name： | 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone |
| Inchi Code | 1S/C22H17ClN6O/c1-13(28-21-19-20(25-11-24-19)26-12-27-21)17-10-14-6-5-9-16(23)18(14)22(30)29(17)15-7-3-2-4-8-15/h2-13H,1H3,(H2,24,25,26,27,28)/t13-/m0/s1 |
| Inchi Key | SJVQHLPISAIATJ-ZDUSSCGKSA-N |
安全信息
