CP-724714
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.
CP-724714是一种erbB2和EGFR激酶的抑制剂,IC50值分别为10±3 nM和6,400±2,100 nM[1]。
在体外细胞周期实验中,CP-724714可抑制erbB2,引起Her2扩增BT-474乳腺癌细胞的G1期停滞。1 mol/L的CP-724714也能在这些细胞中减少磷酸化erbB2的水平。
在体内实验中,CP-724714可在携带FRE-erbB2异种移植物的无胸腺小鼠中导致浓度依赖的肿瘤erbB2受体磷酸化水平下降。CP-724714疗法也可时间和剂量依赖地引起肿瘤细胞凋亡。在两种Her2扩增并过表达erbB2的人类乳腺癌模型BT-474和MDA-MB-453中,CP-724714对异种移植物的生长存在剂量依赖的抑制。此外,CP-724714疗法可引发下游erbB2 RTK信号减弱。基于此,CP-724714已发展到I期临床试验,也是Her2引发的乳腺癌的潜在药物选择[1]。
参考文献:
[1] Jitesh P. Jani, Richard S. Finn, Mary Campbell, et al. Discovery and Pharmacologic Characterization of CP-724714, a Selective ErbB2 Tyrosine Kinase Inhibitor. Cancer Research. 2007 (67): 9887-9893.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 469.53 |
Cas No. | 537705-08-1 |
Formula | C27H27N5O3 |
Solubility | ≥23.5 mg/mL in DMSO; insoluble in H2O; ≥25.4 mg/mL in EtOH |
Chemical Name | 2-methoxy-N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide |
SDF | Download SDF |
Canonical SMILES | CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C |
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 | CP-724714是一种erbB2和EGFR激酶的抑制剂,IC50值分别为10±3 nM和6,400±2,100 nM。 | |||||
靶点 | erbB2 | EGFR | ||||
IC50 | 10±3 nM | 6,400±2,100 nM |