Abexinostat
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Cat.No：IA1710 Solarbio
CAS：783355-60-2
Storage：Powder:2-8℃，2 years
Purity：≥98%
Appearance：Light yellow to yellow Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > Abexinostat
Product Information
| CAS | 783355-60-2 |
| Name | Abexinostat |
| Molecular Formula | C21H23N3O5 |
| Molecular Weight | 397.42 |
| Solubility | Soluble in --- |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years |
| EC | EINECS 811-183-9 |
| MDL | MFCD10565969 |
| SMILES | O=C(NCCOC1=CC=C(C=C1)C(NO)=O)C2=C(C3=CC=CC=C3O2)CN(C)C |
| Target Point | HDAC |
| Passage | DNA Damage/DNA Repair;Epigenetics;NF-κB |
| Background | Abexinostat/PCI-24781 is a novel pan-HDAC inhibitor. |
| Biological Activity | Abexinostat是一种新的泛HDAC抑制剂，主要靶向HDAC1的Ki值为7 nM[1-3]。 |
| In Vitro | Abexinostat(CRA 024781)对多种肿瘤细胞系显示出有效的抗肿瘤活性，GI50％范围为0.15μM至3.09μM。 Abexinostat(CRA 024781)对HUVEC内皮细胞也具有抗增殖作用，GI50％为0.43μM。 Abexinostat(CRA 024781)处理导致HCT116或DLD-1细胞中乙酰化组蛋白和乙酰化微管蛋白的剂量依赖性积累，诱导p21的表达，并导致PARP裂解和γH2AX的积累[1]。 Abexinostat(CRA 024781)对HDAC酶的抑制导致与HR特异性相关的基因(包括RAD51)的转录显着减少。与HR的抑制一致，Abexinostat(CRA 024781)处理导致在转染的CHO细胞中进行I-SceI诱导的染色体断裂的同源定向修复的能力降低[2]。 Abexinostat(CRA 024781)在软组织肉瘤(STS)细胞中诱导S期耗竭，G2细胞周期停滞和细胞凋亡。 Abexinostat(CRA 024781)在STS细胞中诱导Rad51转录抑制，可能通过增强的E2F1与Rad51近端启动子结合而介导[3]。 |
| In Vivo | 对携带HCT116或DLD-1结肠肿瘤异种移植物的小鼠肠胃外施用Abexinostat(CRA 024781)导致肿瘤生长的统计学显着降低。抑制肿瘤生长伴随着外周血单核细胞中α-微管蛋白乙酰化的增加，以及肿瘤中许多基因表达的改变，包括一些参与凋亡和细胞生长的基因[1]。 |
| Cell Experiment | 将10个肿瘤细胞系和HUVEC培养至少两倍，并在化合物暴露结束时使用Alamar蓝荧光细胞增殖测定监测生长。使用范围为0.0015至10μmol/ L的半对数间隔，在96孔板中以9个浓度在一式三份孔中测定化合物。每个孔中的最终DMSO浓度为0.15％。使用四参数逻辑方程[1]通过非线性回归估计抑制细胞生长50％和95％置信区间所需的浓度。 |
| Animal Experiment | 将HCT116和DLD-1肿瘤细胞皮下植入雌性BALB / c nu / nu小鼠中，每只小鼠3×106。当平均肿瘤体积为-100 mm时，开始用Abexinostat(CRA 024781)治疗[1]。携带人结肠肿瘤异种移植物的小鼠用Abexinostat(CRA 024781)静脉内给药，使用各种剂量和方案评估Abexinostat(CRA 024781)的抗肿瘤活性[1]。 |
| Data Literature Source | [1]. Buggy JJ， et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther， 2006， 5 (5) ， 1309-1317. [2]. Adimoolam S， et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A， 2007， 104 (49) ， 19482-19487. [3]. Lopez G， et al. Combining PCI-24781， a novel histone deacetylase inhibitor， with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res， 2009， 15 (10) ， 3472-3483. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
是一种新的泛HDAC抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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