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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PIKfyve-HZX-02-059
HZX-02-059

Chemical Structure : HZX-02-059

CAS No.: 2240205-30-3

HZX-02-059 (Methuosis inducer 1)

货号: PC-47003Not For Human Use, Lab Use Only.

HZX-02-059 is a PIKfyve and tubulin dual-target inhibitor with high affinity for PIKfyve (Kd=10.4 nM), HZX-02-059 is a potent methuosis inducer, shows both in vitro and in vivo anti-tumor activity against TNBC.

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5 mg ¥1980 In stock
10 mg ¥2980 In stock
25 mg ¥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HZX-02-059 (Methuosis inducer 1) is a PIKfyve and tubulin dual-target inhibitor with high affinity for PIKfyve (Kd=10.4 nM), HZX-02-059 is a potent methuosis inducer, shows both in vitro and in vivo anti-tumor activity against TNBC.
HZX-02-059 exerts anti-proliferative action of DHL cells in a dose- and time-dependent manner, including Will-2, LR, and TMD8 cells (IC50=150-350 nM, 48 h).
HZX-02-059 induces a caspase-independent cell death in DHL cells. HZX-02-059 triggers non-apoptotic cell death of methuosis as a result of PIKfyve/TFEB inhibition.
HZX-02-059-induced cell cycle arrest is mechanistically associated with the inhibition of tubulin and mTOR/Myc axis.
HZX-02-059 (20 mg/kg, i.p.) suppresses growth of xenograft derived from DHL cells with a low systemic toxicity profile.

物理化学性质&存储条件

分子量 487.486
分子式 C27H20F3N5O
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

N-(4-methyl-3-((6-(pyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)amino)phenyl)-3-(trifluoromethyl)benzamide

参考文献

1. Liying Feng, et al. Cell Death Discov. 2022 Jan 28;8(1):39.

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