ARRY 520 trifluoroacetate
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.
ARRY 520 trifluoroacetate是合成的KSP抑制剂的盐形式,IC50值为6 nM。
驱动蛋白纺锤体蛋白(KSP)是一种有丝分裂驱动蛋白,参与有丝分裂早期阶段的中心体分离。
体外实验:在各种肿瘤细胞系中,ARRY-520具有低纳摩尔的抗增殖活性,对多药耐药细胞系也具有活性。ARRY-520抑制HCT-15、NCI/ADR-RES和K562 / ADR细胞增殖的EC50分别为3.7、14和4.2 nM,而这些细胞系中紫杉醇的EC50为35、565和372 nM。与母体K562细胞系相比,K562 / ADR对紫杉醇具有118倍的耐受性,而对ARRY-520的耐受性仅为3.5倍[1]。
在体实验:在对紫杉醇完全耐受的UISO-BCA-1异种移植模型中,ARRY-520具有活性。在HT-29、HCT-116、MDA-MB-231和A2780异种移植小鼠模型中,ARRY-520的抗肿瘤效果优于紫杉醇。在雄激素受体阴性前列腺癌PC-3和DU145前列腺癌异种移植模型中,ARRY-520的效果优于多西他赛(docetaxel)[1]。
临床试验:I期临床试验确定了ARRY-520的安全性和最大耐受剂量(MTD)。两个剂量方案的每个循环的总剂量MTD为4.5 mg/m2。剂量限制性毒性反应包括皮疹脱落、手足综合征、粘膜炎和高胆红素血症。36个患者中,有33个患者出现3级或4级的可逆的药物相关的骨髓抑制[2]。
参考文献:
[1] Woessner R, Tunquist B, Lemieux C, Chlipala E, Jackinsky S, Dewolf W Jr, Voegtli W, Cox A, Rana S, Lee P, Walker D. ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 2009;29(11):4373-80.
[2] Khoury HJ, Garcia-Manero G, Borthakur G, Kadia T, Foudray MC, Arellano M, Langston A, Bethelmie-Bryan B, Rush S, Litwiler K, Karan S, Simmons H, Marcus AI, Ptaszynski M, Kantarjian H. A phase 1 dose-escalation study of ARRY-520, a kinesin spindle protein inhibitor, in patients with advanced myeloid leukemias. Cancer. 2012;118(14):3556-64.
Physical Appearance | Off-white solid |
Storage | Store at -20°C |
M.Wt | 420.48 |
Cas No. | 885060-09-3 |
Formula | C20H22F2N4O2S·CF3CO2H |
Solubility | Soluble in DMSO |
Chemical Name | (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN(C(=O)N1C(SC(=N1)C2=C(C=CC(=C2)F)F)(CCCN)C3=CC=CC=C3)OC |
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。 |