Imexon

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

一种 2-氰基氮丙啶衍生物，对某些类型的癌症具有抗肿瘤活性。

A 2-cyanoaziridine derivative with antitumor activity in some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma; induces mitochondrial oxidation and induces apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8; an apoptosis inducer agent.Blood Cancer Phase 2 Clinical.

Imexon (BM 06002) induces oxidative stress in the ER, activates an ER stress response. Imexon (BM 06002) does not significantly alter the levels of eIF2B5, however there is a dose-dependent increase in the phosphorylation of eIF2alpha, as well as an increase in the levels of GTP exchange protein eIF2B2 in MiaPaCa-2, Panc-1, and BxPC3 cells. Imexon (BM 06002) induces single-stranded breaks in the human A375 melanoma cells but only significantly at the highest concentrations for each agent compared to controls. Imexon plus DTIC cytotoxicity is additive. Imexon (BM 06002) show inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, with IC50s of 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM.

Imexon (BM 06002) in combination with DTIC results in an increase in the peak plasma imexon level in non-tumor-bearing mice. The combination of both drugs increases plasma imexon AUC by 22% (p=0.026). Imexon (BM 06002) (100 mg/kg/day, i.v.) treatment decreases the body weight of SCID mice bearing human A375 melanoma tumors, but there is no significant difference in tumor growth. Imexon (BM 06002) (100 mg/kg) in combination with GEM shows synergistic inhibition of Panc-1 tumor growth in SCID mice.

Amplimexon | BM 06002

Apoptosis

Apoptosis

Apoptosis

Cancer

Blood cancer

59643-91-3

111.104

C4H5N3O

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (562.56 mM)

O=C1N2CC2C(N)=N1

4-Amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one

(-20℃)

With Ice Pack

≥ 2 years