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谢尔德梅坦(JNJ-26854165)

谢尔德梅坦(JNJ-26854165)用途

Serdemetan(JNJ-26854165)是HDM2泛素连接酶拮抗剂,能诱导p53野生型细胞的早期凋亡。

谢尔德梅坦(JNJ-26854165)名称

[ CAS 号 ]:
881202-45-5

[ 中文名 ]:
N-[2-(1H-吲哚-3-基)乙基]-N’-(4-吡啶基)-1,4-苯二胺

[ 英文名 ]:
Serdemetan

[英文别名 ]:

Serdemetan
JNJ 26854165

谢尔德梅坦(JNJ-26854165)生物活性

[ 描述 ]:

Serdemetan(JNJ-26854165)是HDM2泛素连接酶拮抗剂,能诱导p53野生型细胞的早期凋亡。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> MDM-2/p53

研究领域 >> 癌症

[参考文献]

[1]. T. Stühmer et al. A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo Journal of Clinical Oncology, 2008 ASCO Annual Meeting Proceedings (Post-Meeting Edition ).Vol 26, No 15S (May 20 Supplement), 2008: 14694

[2]. Chargari C, Leteur C, Angevin E, Bashir T, Schoentjes B, Arts J, Janicot M, Bourhis J, Deutsch E.Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.Cancer Lett. 2011 Dec 22;312(2):209-18.

[3]. Smith MA, Gorlick R, Kolb EA, Lock R, Carol H, Maris JM, Keir ST, Morton CL, Reynolds CP, Kang MH, Arts J, Bashir T, Janicot M, Kurmasheva RT, Houghton PJ.Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.Pediatr Blood Cancer. 2012 Aug;59(2):329-32.

[4]. Tabernero J, Dirix L, Sch?ffski P, Cervantes A, Lopez-Martin JA, Capdevila J, van Beijsterveldt L, Platero S, Hall B, Yuan Z, Knoblauch R, Zhuang SH.A phase I first-in-human pharmacokinetic and pharmacodynamic study of serdemetan in patients with advanced solid tumors.Clin Cancer Res. 2011 Oct 1;17(19):6313-21. Epub 2011 Aug 10.

[5]. Kojima K, Burks JK, Arts J, Andreeff M.The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias.Mol Cancer Ther. 2010 Sep;9(9):2545-57. Epub 2010 Aug 24.

[相关活性小分子]

谢尔德梅坦(JNJ-26854165)物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
615.1±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₁H₂₀N₄

[ 分子量 ]:
328.410

[ 闪点 ]:
325.8±30.1 °C

[ 精确质量 ]:
328.168793

[ PSA ]:
52.74000

[ LogP ]:
3.45

[ 外观性状 ]:
brown solid

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.747

[ 储存条件 ]:
-20℃

谢尔德梅坦(JNJ-26854165)安全信息

[ 海关编码 ]:
2933990090

谢尔德梅坦(JNJ-26854165)海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%