CX-6258
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.
Pim激酶(Moloney鼠白血病病毒的原病毒整合位点)是调节细胞存活的丝氨酸/苏氨酸激酶家族。该激酶家族由三个不同的亚型(PIM-1、PIM-2和PIM-3)组成。同时抑制PIM-1、PIM-2和PIM-3激酶正成为开发抗癌药物的一个有希望的策略。CX-6258是一种强效的、选择性的和口服有效的pan-Pim激酶抑制剂。
体外:CX-6258体外表现出与化疗药物的协同作用。针对一组来自人实体瘤和血液恶性肿瘤的细胞系,检查了CX-6258的抗增殖活性。CX-6258对所测试的所有细胞系表现出强效的抑制增殖效力[1]。
体内:在急性骨髓性白血病MV-4-11和前列腺癌PC3两个人类肿瘤异种移植生长功效模型中评价CX-6258。该药物表现出剂量依赖性功效,用50 mg/kg剂量产生45%的肿瘤生长抑制(TGI),100 mg/kg剂量产生75%的TGI。此外,CX-6258在代表疾病的两个异种移植物模型中显示出显著功效,已被证明这些疾病中Pim激酶可发挥重要作用[1]。
临床试验:没有临床数据可用。
参考文献:
[1] Haddach M, Michaux J, Schwaebe MK, et al. Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011;3(2):135-9.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 461.94 |
Cas No. | 1202916-90-2 |
Formula | C26H24ClN3O3 |
Synonyms | CX6258;CX 6258 |
Solubility | insoluble in EtOH; ≥11.15 mg/mL in DMSO; ≥2.575 mg/mL in H2O with gentle warming |
Chemical Name | (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one |
SDF | Download SDF |
Canonical SMILES | CN1CCCN(C(C2=CC(C3=CC=C(/C=C4C(C=C(Cl)C=C5)=C5NC\4=O)O3)=CC=C2)=O)CC1 |
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。 |
Description | CX-6258 HCl是一种强效的、口服有效的pan-Pim激酶抑制剂,作用于Pim1、 Pim2和Pim3的IC50值分别为5 nM、25 nM和16 nM。 | |||||
靶点 | Pim1 | Pim3 | Pim2 | |||
IC50 | 5 nM | 16 nM | 25 nM |
质量控制和MSDS
- 批次: