1. PI3K/Akt/mTOR
  2. PI3K
  3. PI3kδ inhibitor 1

PI3kδ inhibitor 1 

Cat. No.: HY-15288
Handling Instructions

PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.

For research use only. We do not sell to patients.

PI3kδ inhibitor 1 Chemical Structure

PI3kδ inhibitor 1 Chemical Structure

CAS No. : 1332075-63-4

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.

IC50 & Target[3]

PI3Kδ

3.8 nM (IC50)

In Vitro

PI3kδ inhibitor 1 (Compound 3) is a potent inhibitor of PI3Kδ that is 200-400 fold selective for all three remaining Class I PI3K isoforms and extremely selective relative to 239 kinases tested in SelectScreen service (0/239 kinases showing >50% inhibition when tested at 1 μM; mTOR, DNA-PK, VPS34, PI4Kα and PI4Kβ are inhibited at 10% or less when tested at 1 μM; PIKC2A and PIKC2B are inhibited at 11% and 42%, respectively, at this same concentration and show less than 10% inhibition when tested at 0.1 μM; the PIKK family kinases ATM and ATR are not assessed)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The pharmacokinetic properties of PI3kδ inhibitor 1 (Compound 3) are evaluated in mice and rats when dosed IV and orally. Good plasma exposures and reasonable half-lives are observed upon oral dosing, a reflection of high oral bioavailability (80% and 90% at a low dose for mouse and rat, respectively), moderate volume of distribution, and moderate clearance. PI3kδ inhibitor 1 has moderate terminal elimination half-life (t1/2=2.6 h, 2.9 h, 5 h, 2.6, 3.8 and 4.8 h for mouse (5 mg/kg, po), mouse (20 mg/kg, po), mouse (40 mg/kg, po), rat (5 mg/kg, po), rat (10 mg/kg, po), rat (30 mg/kg, po)). Plasma exposures and Cmax levels increase with dose in both mice and rats, important in that inflammatory disease models utilize these two species. Plasma protein binding for PI3kδ inhibitor 1 ranges from 80-88% in rodents and is consistent with values obtained in human plasma (86%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

504.60

Formula

C₂₈H₃₃FN₆O₂

CAS No.

1332075-63-4

SMILES

CC(O)(C1CCN(CC2=NC3=C(N4CCOCC4)N=C(C5=C(F)C=CC6=C5C=CN6)N=C3C=C2)CC1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[1]

Mice and Rats[1]
Female mice are dosed IV (intravenously) with PI3kδ inhibitor 1 in 5% DMSO/5% Cremephor and PO (orally) as an MCT suspension (0.5% methylcellulose/0.2% Tween-80). The IV (1 mg/kg) and PO (5, 20 and 40 mg/kg) studies are performed in CD-1 mice while the higher dose studies are performed in the Balb/c strain. Male Sprague-Dawley rats are dosed with the same IV (1 mg/kg) and PO (5, 10 and 30 mg/kg) formulations as those used for mice.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PI3kδ inhibitor 1PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PI3kδ inhibitor 1
Cat. No.:
HY-15288
Quantity:
MCE Japan Authorized Agent: