PI3Kδ-IN-1 是高效，选择性的 PI3Kδ 抑制剂，IC50 为 1.7 nM。
货号:ajcx39112
CAS:1911564-39-0
分子式:C22H20F3N7O2
分子量：471.44
溶解度:DMSO : 62.5 mg/mL (132.57 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

PI3Kδ-IN-1 (compound 52) shows >100-fold selectivity over the other PI3K isoforms. Kinome selectivity is also excellent with >660-fold selectivity over MNK1 and others in HTRF assays. Importantly, PI3Kδ-IN-1 has an improved human/rodent in vitro stability correlation and a good permeability profile[1].

PI3Kδ-IN-1 (2, 5 mg/kg, orally b.i.d. for 42 days) shows greater than 50% suppression of paw swelling in mice. PI3Kδ-IN-1 has an EC50 of 10 nM at 24 h (ED50 of ∼1.25 mg/kg) in mice[1].

[1]. Liu Q, et al. Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. J Med Chem. 2017 Jun 22;60(12):5193-5208.