| CAS NO: | 548472-68-0 |
| 规格: | 98% |
| 分子量: | 581.49 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
Background:
(±)-Nutlin-3 is a potent and selective MDM2 antagonist with IC50 value of 0.09 μM [1].
Mouse double minute 2 homolog (MDM2) is an important negative regulator of p53, a tumor suppressor. Disruption of the p53-MDM2 interaction can lead to the activation of p53 and tumor growth inhibition [1].
(±)-Nutlin-3 is a potent and selective MDM2 antagonist. In both normal and leukemic B cells, Nutlin-3 induced accumulation of p53 protein in a dose-dependent way. In B-CLL cells, Nutlin-3 also induced cell death with IC50 value of 10.4 μM and induced the transcription of p53 target genes, such as PCNA, CDKN1A/p21, GDF15, TNFRSF10B/TRAIL-R2, TP53I3/PIG3, GADD45, and DDB1 [2].
In mice bearing subcutaneous human cancer xenografts (SJSA-1), Nutlin-3 (200 mg/kg) orally treated twice a day for 20 days inhibited tumor growth by 90% [1]. In mice with established UKF-NB-3rDOX20 xenografts, Nutlin-3 (200 mg/kg) increased caspase-3 activity and induced apoptosis [3].
参考文献:
[1].Shinohara T, Uesugi M.? In-vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Tanpakushitsu Kakusan Koso. 2007 Oct;52(13 Suppl):1816-7.
[2].Secchiero P, Barbarotto E, Tiribelli M, et al.? Functional integrity of the p53-mediated apoptotic pathway induced by the nongenotoxic agent nutlin-3 in B-cell chronic lymphocytic leukemia (B-CLL). Blood. 2006 May 15;107(10):4122-9.
[3].Van Maerken T, Ferdinande L, Taildeman J, et al.? Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53. J Natl Cancer Inst. 2009 Nov 18;101(22):1562-74.
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