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PI3Kδ-IN-1

Names

[ CAS No. ]:
1911564-39-0

[ Name ]:
PI3Kδ-IN-1

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Research Areas >> Inflammation/Immunology

[Target]

IC50: 1.7 nM (PI3Kδ)[1]


[In Vitro]

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].

[In Vivo]

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]. Animal Model: Male DBA/1 mice (20−25g)[1] Dosage: 0.5, 2, 5 mg/kg Administration: Oral b.i.d. for 42 days, Result: A dose dependent reduction of the clinical score was observed. Doses of 2 and 5 mg/kg showed greater than 50% suppression of paw swelling[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20F3N7O2

[ Molecular Weight ]:
471.44

Related Compounds