| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 10mg | 询价 |
| 50mg | 询价 |
| 200mg | 询价 |
Cell lines | Mouse NIH/3T3 fibroblasts |
Preparation Method | Exponentially growing mouse NIH/3T3 fibroblasts (wt-TP53) were incubated for 7 days in the presence of Nutlin-3a chiral and stained live by acridine orange. |
Reaction Conditions | 10 μM Nutlin-3a chiral for 7 days |
Applications | When tested the activity of Nutlin-3a chiral, on exponentially proliferating mouse NIH/3T3 fibroblasts that express wild-type p53, Seven days of incubation with 10 μM Nutlin-3a chiral led to >90% inhibition of NIH/3T3 cells growth. |
Animal models | Sjsa-1 tumor-bearing nude mice |
Preparation Method | Mice were given an oral dose of 200 mg/kg Nutlin-3a chiral twice daily for 2 weeks (LnCaP and 22Rv1) or 3 weeks (MHM) |
Dosage form | 200mg/kg Nutlin-3a chiral for 2 or 3 weeks |
Applications | Nutlin-3a chiral inhibited xenograft growth in a dose-dependent manner, with the highest dose (200 mg/kg) showing significant tumor shrinkage |
| 产品描述 | Nutlin-3a chiral, an active isomer of Nutlin-3, is a murine double microbody 2 (MDM2) antagonist with IC50 value of 0.09μM . Nutlin-3a chiral inhibits MDM2-p53 interaction and activates wild-type p53, inducing cell cycle arrest and apoptosis[2]. Incubation with 10 μm Nutlin-3a chiral for 7 days resulted in > 90% inhibition of NIH/3T3 cell growth but did not affect MEF proliferation, in which both targets of the drug were eliminated[3]. Nutlin-3a chiral was able to increase the sensitivity to BBR and certain NAX compounds. The effects of Nutlin-3a chiral were usually more substantial in those cells containing an introduced WT TP53 gene[6]. Nutlin-3a chiral binds MDM2 in the TP53-bindingpocket, thereby interfering with MDM2-directed TP53 degradation. This has been shown to cause cell cycle arrest, growth inhibitionand apoptosis in both solid tumors and lymphoid neoplasms.In mantle cell lymphoma(MCL), Nutlin-3a chiral can inhibit cell growth and activate apoptosis in bothwt-TP53(IC50 of 1 to 10μM) and mt-TP53(IC50 of 22.5μM) cells[4]. Nutlin-3a chiral can also effectcell cycle in gastric cancer cell lines. It induces G1 arrest inMKN-45 and SNU-1 cell lines[5].LA-N-5(human neuroblastoma) and SMS-KCNR cells pretreated with Nutlin-3a chiral were significantly more susceptible to DNAM-1-engineered NK cells than NK cells transfected with the empty vector suggesting that the combined use of DNAM-1-chimeric receptor-engineered NK cells and Nutlin-3a chiral may represent a novel therapeutic approach for the treatment of solid tumors, such as NB, carrying dysfunctional p53[7]. In Sjsa-1 tumor-bearing nude mice, Nutlin-3a chiral inhibited xenograft growth in a dose-dependent manner, with the highest dose (200 mg/kg) showing significant tumor shrinkage[3]. References: |
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