ON 146040

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ON 146040 是一种有效的 PI3K 同工型抑制剂，对 PI3Kα 和 PI3Kδ 的 IC50 值分别为 14 和 20 nM。

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

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.

——

ZINC211117138

PI3K/Akt/mTOR signaling

PI3K

CB1

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years