Description
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.
Product information
CAS Number: 1821038-80-5
Molecular Weight: 416.49
Formula: C20H24N4O4S
Chemical Name: 3-[6-amino-5-(2-methyl-1,3-oxazol-5-yl)pyridin-3-yl]-N-(2-hydroxy-2-methylpropyl)-4-methylbenzene-1-sulfonamide
Smiles: CC1=CC=C(C=C1C1C=C(C(N)=NC=1)C1=CN=C(C)O1)S(=O)(=O)NCC(C)(C)O
InChiKey: UQIUWUJYJBQZBY-UHFFFAOYSA-N
InChi: InChI=1S/C20H24N4O4S/c1-12-5-6-15(29(26,27)24-11-20(3,4)25)8-16(12)14-7-17(19(21)23-9-14)18-10-22-13(2)28-18/h5-10,24-25H,11H2,1-4H3,(H2,21,23)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PI3Kγ inhibitor 4 inhibits PI3Kγ and PI3Kα in U937 cells, with IC50s of 120 nM and 6250 nM, respectively.
In Vivo:
PI3Kγ inhibitor 4 (10-20 mg/kg; a single p.o.) dose dependently inhibits the amplitude of the enhanced pause (ΔPenh) response to ovalbumin in a model of airway inflammation. PI3Kγ inhibitor 4 (a single p.o.) exhibits high oral bioavailability (72, 94 and 122%) and Cmax (1.53, 12.2 and 25.2 μM) following oral administration (10, 100 and 300 mg/kg) in rats.
Products are for research use only. Not for human use.
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