IHMT-PI3Kδ-372 

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56～83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research^[1].

IHMT-PI3Kδ-372 (Compound (S)-18; 0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC₅₀ value of 67 nM^[1].
IHMT-PI3Kδ-372 (compound (S)-18) shows moderate inhibition of CYP2C9 (IC₅₀ of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC₅₀s > 10 μM)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IHMT-PI3Kδ-372 (Compound (S)-18; 1-5 mg/kg; inhalation; daily; for 28 days) improves lung function and reduced the inflammatory patterns characteristic of COPD. The lung function parameters such as forced expiratory volume in the first second (FEV1), forced vital capacity (FVC), and peak expiratory flow (PEF) are improved dose-dependently. The abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes are also reduced. IHMT-PI3Kδ-372 decreases the inflammatory cell infiltration in a dose-dependent manner^[1].
In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (compound (S)-18) displays a half-life of 2.3 h, low exposure of 66 ng/mL, and high clearance of 348.5 mL/min/kg in plasma but high exposure of 5599 ng/g (6 h after inhalation) in lung tissue^[1].
IHMT-PI3Kδ-372 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

503.50

C₂₆H₂₃F₂N₇O₂

2429889-61-0

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Feng Li, et al. Discovery of (S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1 H-pyrazolo[3,4- d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3 H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease. J Med Chem. 2020 Nov 25;63(22):13973-13993.  [Content Brief]