Selective PI3Kδ Inhibitor 1 (compound 7n)

Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].

Selective PI3Kδ Inhibitor 1 (compound 7n) Chemical Structure

Selective PI3Kδ Inhibitor 1 (compound 7n) Chemical Structure

CAS No. 2088525-31-7

Purity & Quality Control

Selective PI3Kδ Inhibitor 1 (compound 7n) Related Products

Signaling Pathway

Biological Activity

Description Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
Targets
PI3Kδ [1]
(Cell-free assay)
0.9 nM
In Vivo
In vivo

The compound shows reasonable pharmacokinetics with good bioavailability and moderate in vivo half-life. In rats, the oral bioavailability (F%) is 41, the Vss, T1/2 and CL are 2.8 L/kg, 3.4 h and 12 mL/min/kg respectively after IV administration[1].

Chemical Information & Solubility

Molecular Weight 429.45 Formula

C23H20FN7O

CAS No. 2088525-31-7 SDF --
Smiles CN1C(=NC(=N1)C2=CN=C(C(=N2)C3=CC(=C(C=C3)C(=O)N)F)N)C4(CC4)C5=CC=CC=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 43 mg/mL ( (100.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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