PI3Kδ inhibitor 52

Research use only, not for human use.

A potent, selective, and efficacious PI3Kδ inhibitor with IC50 of 1.7 nM.

A potent, selective, and efficacious PI3Kδ inhibitor with IC50 of 1.7 nM, >100-fold selectivitity over PI3Kγ/α/β; shows potent activity in mouse arthritis models.

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.

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. Animal Model:Male DBA/1 mice (20?25g)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.

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PI3K/Akt/mTOR signaling

PI3K

PI3K

Inflammation/Immunology

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1911564-39-0

471.444

C22H20F3N7O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (132.57 mM)

CC(=O)N1CCN(C(=O)C1(C)C)C2=C(C=CC(=C2)C3=CC(=C4N3N=CN=C4N)C(F)(F)F)C#N

2-(4-acetyl-3,3-dimethyl-2-oxopiperazin-1-yl)-4-(4-amino-5-(trifluoromethyl)pyrrolo[2,1-f][1,2,4]triazin-7-yl)benzonitrile

(-20℃)

With Ice Pack

≥ 2 years