CAS NO: | 1911564-39-0 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 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) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. |