1. PI3K/Akt/mTOR
    Protein Tyrosine Kinase/RTK
  2. PI3K
    Bcr-Abl
  3. ON 146040

ON 146040 

Cat. No.: HY-12338
Handling Instructions

ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).

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

ON 146040 Chemical Structure

ON 146040 Chemical Structure

CAS No. : 1404231-34-0

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Description

ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).

IC50 & Target[1]

PI3Kα

14 nM (IC50)

PI3Kδ

20 nM (IC50)

PI3Kγ

1 μM (IC50)

PI3Kβ

3 μM (IC50)

Abl1

150 nM (IC50)

In Vitro

In biochemical testing, ON 146040 inhibits PI3Kα/ PI3Kδ isoforms (IC50≈14 and 20 nM, respectively) without having a major effect on PI3Kβ/ PI3Kγ isoforms (IC50≈3 and 1 μM, respectively). ON 146040 is also found to inhibit Abl1 and several mutant versions of this kinase (IC50<150 nM), although ON 146040 is not found to be active against the T315I mutant. ON 146040 represents the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways. ON 146040 disrupts the oncogenic activity of both STAT3 and STAT5 by targeting upstream activators, including PI3K α and δ isoforms as well as wild type and mutant BCR-ABL. ON 146040 is highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation are down-regulated in leukemia and myeloma cells[1].

Molecular Weight

489.55

Formula

C₂₄H₂₃N₇O₃S

CAS No.

1404231-34-0

SMILES

CN(CC1)CCN1C(C=C2)=CC=C2NC3=NC(S/C(C(N4)=O)=C\C5=CC=C([N+]([O-])=O)C=C5)=C4C=N3

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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Keywords:

ON 146040ON146040ON-146040PI3KBcr-AblPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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