CAS NO: | 881202-45-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces earlyapoptosisin p53 wild-type cells, inhibits cellular proliferation followed by delayedapoptosisin the absence of functional p53. IC50 value: HDM2 ubiquitin ligase Target: in vitro: JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and inducesapoptosisin leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferentialapoptosisof S-phase cells. JNJ 26854165 is an oralMdm2 inhibitorwhich can inhibit the interaction of Mdm2-p53 complex with theproteasomeand increase p53 levels by binding to RING domain ofMdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four humancancercell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. in vivo:JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 328.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H20N4 | ||||||||||||||||
CAS 号 | 881202-45-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(152.25 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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