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Selective PI3Kδ Inhibitor 1

Product Name
Selective PI3Kδ Inhibitor 1
CAS No.
2088525-31-7
Chemical Name
Selective PI3Kδ Inhibitor 1
Synonyms
PI3Kδ-IN-5;compound 7n;PI3Kδ-IN-7n;PI3K delta-IN-7n;SelectivePI3KδInhibitor1;Selective PI3Kδ Inhibitor 1;SelectivePI3KδInhibitor1(compound7n);SELECTIVE PI3KΔ INHIBITOR 1;COMPOUND 7N;4-(3-Amino-6-(1-methyl-5-(1-phenylcyclopropyl)-1H-1,2,4-triazol-3-yl)pyrazin-2-yl)-2-fluorobenzamide;Benzamide, 4-[3-amino-6-[1-methyl-5-(1-phenylcyclopropyl)-1H-1,2,4-triazol-3-yl]-2-pyrazinyl]-2-fluoro-
CBNumber
CB23379666
Molecular Formula
C23H20FN7O
Formula Weight
429.45
MOL File
2088525-31-7.mol
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Selective PI3Kδ Inhibitor 1 Property

storage temp. 
Store at -20°C
solubility 
DMSO: 43 mg/mL (100.13 mM);Ethanol: Insoluble
form 
Solid
color 
Off-white to gray
Water Solubility 
Water: Insoluble
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Hazard and Precautionary Statements (GHS)

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Selective PI3Kδ Inhibitor 1 Chemical Properties,Usage,Production

Uses

PI3Kδ-IN-5 (compound 7n) is a highly potent and selective inhibitor of PI3Kδ with an IC50 of 0.9 nM[1].

Biological Activity

Selective PI3Kδ Inhibitor 1 (compound 7n) is a PI3Kδ inhibitor with IC50 of 0.9 nM for PI3Kδ, which is more than 1000-fold selective for other class I PI3K isoforms. The IC50 values of it for PI3Kα/γ/β were 3670, 1460, and 21300 nM, respectively.

in vivo

Selective PI3Kδ Inhibitor 1 has favorable pharmacokinetic profile: good bioavailability and moderate in vivo half-life. In rats, its oral bioavailability was 41%; after intravenous injection, Vss, T 1/2 and CL were 2.8 L/kg, 3.4 h and 12 mL/min/kg, respectively .

target

TargetValue
PI3Kδ
(Cell-free assay)
0.9 nM

References

[1] Terstiege I, et al. Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kδ inhibitors. Bioorg Med Chem Lett. 2017;27(3):679-687. DOI:10.1016/j.bmcl.2016.11.004

Selective PI3Kδ Inhibitor 1 Preparation Products And Raw materials

Raw materials

Preparation Products

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  • 2088525-31-7