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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-ON 146040
ON 146040

Chemical Structure : ON 146040

CAS No.: 1404231-34-0

ON 146040 (ON-146040;ON146040)

货号: PC-42987Not For Human Use, Lab Use Only.

ON 146040 is a potent, dual PI3K/BCR-ABL inhibitor with IC50 of 14/20 nM for PI3Kα/δ , IC50 of 20 nM for BCR/ABL.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ON 146040 is a potent, dual PI3K/BCR-ABL inhibitor with IC50 of 14/20 nM for PI3Kα/δ , IC50 of 20 nM for BCR/ABL.
ON 146040 displays no significant effect on PI3Kβ/γ isoforms (IC50=3/1 uM), also inhibits Abl1 and several mutant versions of Abl (IC50<150 nM) but not the T315I mutant.
ON 146040 abrogates the oncogenic signaling of STAT3 and STAT5.
ON 146040 is highly potent in killing hematologic tumor cells with IC50 values of 150-1,000 nM, down-regulates STAT3 and STAT5 phosphorylation in leukemia and myeloma cells.

物理化学性质&存储条件

分子量 489.5495
分子式 C24H23N7O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5H-Pyrimido[4,5-b][1,4]thiazin-6(7H)-one, 2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-7-[(4-nitrophenyl)methylene]-

参考文献

1. Stephen Cosenza, et al. Targeting oncogenic STAT3 and STAT5 signaling with on 146040, a small molecule inhibitor of PI3K α/δ and BCR-ABL.

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