1. PI3K/Akt/mTOR
  2. PI3K

PI3Kδ-IN-1 

Cat. No.: HY-101921
Handling Instructions

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

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

PI3Kδ-IN-1 Chemical Structure

PI3Kδ-IN-1 Chemical Structure

CAS No. : 1911564-39-0

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

IC50 & Target

IC50: 1.7 nM (PI3Kδ)[1]

In Vitro

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[1].

In Vivo

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[1].

Animal Model: Male DBA/1 mice (20−25g)[1]
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[1].
References
Molecular Weight

471.44

Formula

C₂₂H₂₀F₃N₇O₂

CAS No.

1911564-39-0

SMILES

NC1=NC=NN2C1=C(C(F)(F)F)C=C2C3=CC=C(C#N)C(N4CCN(C(C)=O)C(C)(C)C4=O)=C3

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PI3Kδ-IN-1
Cat. No.:
HY-101921
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PI3Kδ-IN-1

Cat. No.: HY-101921