CB30865
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.
CB30865是高度有效的细胞毒性剂。该化合物抑制分离的哺乳动物胸苷酸合成酶(TS),但这种抑制作用不足以导致细胞毒性。胸苷酸合成酶(TS)是胸苷酸从头合成(dTTP)的关键酶,被认为是化疗介入的重要靶点。
体外实验:CB30865是最有效的生长抑制剂,在部分小鼠和人类细胞中IC50值范围为1到100 nM。针对W1L2和TS高产的W1L2:C1细胞系,在外源dThd存在情况下,CB300179和CB300189的类似物效价降低。与此相反,CB30865在这些系统中保留活性。等毒性浓度的CB30865处理细胞4-48 h,细胞周期未发生改变[1]。
在体实验:因为水溶性较低(pH 6溶液中小于1 μM),阻碍了CB30865的体内评估。CB30865的低水溶性引发了研究者寻找可以进行体内评价的水溶性类似物。设想可通过在quinazolin-4-one ring引入氨基官能团,例如N-甲基哌嗪,增加其溶解度。
临床试验:没有可用的临床数据。
参考文献:
[1] Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL.? The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. J Med Chem. 2002;45(17):3692-702.
[2] Skelton LA, Ormerod MG, Titley J, Kimbell R, Brunton LA, Jackman AL.? A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. Br J Cancer. 1999;79(11-12):1692-701.
Storage | Store at -20°C |
M.Wt | 516.39 |
Cas No. | 206275-15-2 |
Formula | C26H22BrN5O2 |
Synonyms | ZM242421;CB-30865;CB 30865;ZM-242421;ZM 242421 |
Solubility | Soluble in DMSO |
Chemical Name | 4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide |
SDF | Download SDF |
Canonical SMILES | CC1=NC(=O)C2=CC(=C(C=C2N1)Br)CN(CC#C)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4 |
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。 |