ACY-241
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ACY-241是一种新型的\选择性的和口服有效的HDAC6抑制剂[1][2].
组蛋白去乙酰化酶6(HDAC6)从组蛋白ε-N-乙酰基赖氨酸上移除乙酰基,从而使组蛋白更紧密地包裹DNA.HDAC6在转录调控与细胞周期进程中起着重要作用.
ACY-241是一种新型的\选择性的和口服有效的HDAC6抑制剂.在MM和MCL细胞中,ACY-241与Lenalidomide(len)或Pomalidomide(pom)联合用药可协同增加细胞凋亡,进一步降低转录因子MYC与IRF4表达[1].在多种实体瘤细胞系中,与单一用药相比,
在骨髓瘤细胞异种移植模型中,ACY-241与Pomalidomide联合用药显示出良好的耐受性,无明显的毒性并显著地延长生存期[1].在胰腺癌和卵巢癌异种移植模型中,ACY-241与Paclitaxel联合用药显著地增加具有多极纺锤体的有丝分裂细胞.ACY-241剂量依赖性地增加α-微管蛋白超乙酰化[2].
参考文献:
[1]. Quayle SN, Almeciga-Pinto I, Tamang D, et al. Selective HDAC inhibition by ricolinostat (ACY-1215) or ACY-241 synergizes with IMiD immunomodulatory drugs in Multiple Myeloma (MM) and Mantle Cell Lymphoma (MCL) cells. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research, 2015, Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 5380.
[2]. Huang P, Almeciga-Pinto I, Jordan M, et al. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. In: Proceedings of the 2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; 2015 Nov 5-9; Boston, Massachusetts. Philadelphia (PA): AACR
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 467.95 |
Cas No. | 1316215-12-9 |
Formula | C24H26ClN5O3 |
Solubility | ≥23.4 mg/mL in DMSO; insoluble in H2O; ≥4.87 mg/mL in EtOH with ultrasonic |
Chemical Name | (Z)-2-((2-chlorophenyl)(phenyl)amino)-N-((Z)-7-hydroxy-7-(hydroxyimino)heptyl)pyrimidine-5-carbimidic acid |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=CC=C1N(C2=NC=C(/C(O)=N/CCCCCC/C(O)=N/O)C=N2)C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
A2780卵巢癌细胞 |
溶解方法 |
在DMSO中的溶解度>23.4mg/mL。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 |
0.1、0.3、0.5、1、3μM; 溶于DMSO; 24小时 |
应用 |
在A2780卵巢癌细胞中,ACY-241(0.3μM)增加α-微管蛋白的超乙酰化,与微管蛋白去乙酰化酶HDAC6的抑制一致。 仅在1μM以上的剂量下观察到组蛋白H3的超乙酰化,即I类HDAC的靶标。相对于H3K56,ACY-241优先诱导α-微管蛋白的超乙酰化。 |
动物实验[1]: | |
动物模型 |
携带MiaPaCa-2胰腺癌异种移植物的雌性无胸腺裸鼠 |
剂量 |
ACY-241:50 mg / kg,每日一次,共5天,随后两天休息,连续三周; 腹腔注射紫杉醇:10mg / kg,连续5天; 腹腔注射 |
应用 |
在具有MiaPaCa-2胰腺癌异种移植物的雌性无胸腺裸鼠中,ACY-241(50mg / kg)加紫杉醇(10mg / kg)抑制肿瘤生长,并且不导致体重减轻。作为单一剂量以及与紫杉醇组合时,ACY-241在小鼠中耐受性良好。 |
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]. Huang P, Almeciga-Pinto I, Jordan M, et al. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. In: Proceedings of the 2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; 2015 Nov 5-9; Boston, Massachusetts. Philadelphia (PA): AACR |
质量控制和MSDS
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