产品名称

PX-478 2HCl

一般描述

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor.

别 称

4-[(2S)-2-amino-2-carboxyethyl]-N,N-bis(2-chloroethyl)benzeneamine oxide;dihydrochloride

纯 度

≥98.0%(HPLC)

CAS NO.

685898-44-6

分子式

C¹³H²⁰Cl⁴N²O³

分子量

394.12

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

≥50mg/mL

l  生物学信息

生物活性/药理作用

HIF-1alpha Inhibitor PX-478 is an orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears to inhibit hypoxia-inducible factor 1-alpha (HIF1A)  , which may result in decreased of HIF1A downstream target genes important to tumor growth and survival, a reduction in tumor cell proliferation, and the induction of tumor cell apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor genes VHL and p53 and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1).

应 用

PX-478 is a small molecule inhibitor of hypoxia inducible factor (HIF)-1 alpha currently in a clinical trial in patients with advanced metastatic cancer and lymphoma. PX-478 was effective in models of both non-small cell lung cancer and small cell lung cancer that express HIF-1 alpha.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov