ON 146040

Research use only, not for human use.

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.(In Vitro):ON 146040 inhibits Abl1 and several mutant versions of this kinase with IC50 < 150 nM. ON 146040 is highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1000 nM range. ON 146040 downregulates the phosphorylation of STAT3 and STAT5 in leukemia and myeloma cells.

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.

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ZINC211117138

PI3K/Akt/mTOR signaling

PI3K

CB1

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1404231-34-0

489.55

C24H23N7O3S

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (51.07 mM)

CN1CCN(CC1)c1ccc(Nc2ncc3NC(=O)\C(Sc3n2)=C\c2ccc(cc2)[N+]([O-])=O)cc1

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(-20℃)

With Ice Pack

≥ 2 years