1. PI3K/Akt/mTOR
  2. PI3K
  3. PI3K-IN-2

PI3K-IN-2 

Cat. No.: HY-101517
Handling Instructions

PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).

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

PI3K-IN-2 Chemical Structure

PI3K-IN-2 Chemical Structure

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Description

PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1].

IC50 & Target[1]

PI3Kα

13 nM (IC50)

PI3Kβ

7.1 nM (IC50)

PI3Kδ

190 nM (IC50)

PI3Kγ

8.6 nM (IC50)

In Vitro

PI3K-IN-2 (compound 10) shows PI3Kβ cell IC50 1.1 nM in phosphatase and tensin homolog (PTEN) null MDA-MB-468 cell and PI3Kδ cell IC50 14 nM in Jeko-1 B-cell[1].

In Vivo

PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model[1].

Molecular Weight

525.54

Formula

C₂₈H₂₉F₂N₃O₅

SMILES

O=C1C=C(N2CCOCC2)OC3=C1C=C(C(N4CCCOC4)=O)C=C3[[email protected]@H]5N(C6=CC(F)=CC(F)=C6)CCC5

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

References
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PI3K-IN-2
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HY-101517
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