货号：C0657

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

The important features of cancer cells include uncontrolled cell proliferation, genome instability and mutations, which allow DNA damaging agents to be applied to cancer cells. Cisplatin is such an inorganic platinum complex which can inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin induces formation of DNA adducts which activate several signal transduction pathways, including Erk, p53, p73, and MAPK, which culminates in the activation of apoptosis. The IC50 value of Cisplatin is about 20 μM but vary in different kind of cell types. In HeLa cells, Cisplatin (30 μM) treated for 6 h induces an apparent activation of Erk. Cisplatin also shows an effective antineoplastic activity by inducing tumor cells death. Cisplatin displays ability to cause renal proximal tubular cell (RPTC) apoptosis, causing cell shrinkage, a 50-fold increase in caspase 3 activity, a 4-fold increase in phosphatidylserine externalization, and 5- and 15-fold increases in chromatin condensation and DNA hypoploidy, respectively. In many animal tumors models, like head and neck cancer xenografts, cervical squamous carcinoma xenografts, Cisplatin can also be efficient in regression tumor growth. Cisplatin (5 mg/kg) given weekly i.v. at the day 1 and 7 induces a tumor growth inhibition (GI) of 77.5% and 85.1% of the serous xenografts Ov.Ri(C) and OVCAR-3, respectively. In a neuropathic pain rat model, treated with cisplatin at 2 mg/kg/day produced mechanical allodynia, while it did not induce cold allodynia or thermal hyperalgesia. This dose of cisplatin could work successfully against cancer. In a phase 1 clinical trial, cisplatin was used in treating patients with Non-Small-Cell lung tumors. No dose-limiting toxicities occurred during the first 6 weeks of treatment, Objective response rates for nivolumab 10 mg/kg plus gemcitabine-cisplatin, nivolumab 10 mg/kg plus pemetrexed-cisplatin, nivolumab 10 mg/kg plus paclitaxel-carboplatin, and nivolumab 5mg/kg plus paclitaxel-carboplatin were 33%, 47%, 47% and 43%, respectively; 24-week progression-free survival rates were 51%, 71%, 38%, and 51%, respectively; 2-year OS rates were 25%, 33%, 27%, and 62%, respectively. Responses were achieved regardless of tumor programmed death ligand-1 expression.

作用机制

Reaction with DNA by culminating in either repair of the DNA damage and cell survival or activation of the irreversible apoptotic program.

产品信息