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Resminostat (RAS2410)

现货
Catalog No.
A4108
强效HDAC抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 1,700.00
Ship with 10-15 days
50mg
¥ 5,300.00
Ship with 10-15 days

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Background

Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II (including HDAC1, HDAC3 and HDAC6) with 50% inhibition concentration IC50 values ranging from 43 to 72 nmol/L. Resminostate has the potential to be used for the treatment of multiple myeloma (MM) due to its ability to induce histone H4 hyperacetylation, and apoptosis (IC50 ranging from 2.5 to 3 μmol/L) in MM cells. Recent study results have shown that, in MM cell lines, resminostat abrogates cell growth, suppresses proliferation and induce G0/G1 cell cycle arrest as well as interfering with Akt signaling pathway by decreasing phosphorylation of 4E-BP1 and p70S6k.

Reference

Mandl-Weber S, Meinel FG, Jankowsky R, Oduncu F, Schmidmaier R, Baumann P. The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. Br J Haematol. 2010; 149(4):518-528.

文献引用

1.Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187

Chemical Properties

StorageStore at -20°C
M.Wt349.4
Cas No.864814-88-0
FormulaC16H19N3O4S
SolubilitySoluble in DMSO
Chemical Name(E)-3-[1-[4-[(dimethylamino)methyl]phenyl]sulfonylpyrrol-3-yl]-N-hydroxyprop-2-enamide
SDFDownload SDF
Canonical SMILESCN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(=C2)C=CC(=O)NO
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

OPM-2、NCI-H929、RPMI-8226和U266细胞系

溶解方法

该化合物在DMSO中的溶解度> 10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

5μmol/ L和10μmol/l; 4,24,48,72和96小时

应用

在U266细胞中,Resminostat(RAS2410)导致组蛋白超乙酰化。在人MM细胞系OPM-2,NCI-H929,RPMI-8226和U266细胞系中,Resminostat(10μmol/ l)分别诱导73%,93%,82%和46%的细胞凋亡。Resminostat还强烈地抑制骨髓瘤细胞增殖达92%。

临床实验[2]:

疾病模型

晚期实体瘤患者

剂量

每天一次,每14天的第1-5天给药,剂量范围为100mg至800mg的5个剂量水平; 口服给药

应用

19例晚期实体瘤患者用Resminostat治疗。800mg时,1例患者出现3级恶心和呕吐,2级肝酶升高,1级低钾血症和血小板减少症; 它们是联合剂量限制性毒性(DLT)。HDAC酶的药效学抑制是剂量依赖性的,并且在≥400mg的剂量下达到100%。11例重度预治疗的患者疾病稳定,1例转移性胸腺瘤患者的靶病变尺寸降低了27%。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Mandl-Weber S, Meinel FG, Jankowsky R, Oduncu F, Schmidmaier R, Baumann P. The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. Br J Haematol. 2010; 149(4):518-528.

[2] Brunetto AT1, Ang JE, Lal R, et al. First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2013 Oct 1;19(19):5494-504.

质量控制

质量控制和MSDS

批次:

化学结构

Resminostat (RAS2410)

相关生物数据

Resminostat (RAS2410)