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CAS: 942487-16-3
分子式: C23H25F3N6O2
分子量: 474.48
英文名称: 
pf-03814735
n-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
用途: PF-03814735是一种新型有效的,可逆Aurora A/B抑制剂,IC50为0.8 nM/5 nM,对Flt3, FAK, TrkA作用效果稍弱,对Met和FGFR1具有最低限度的作用活性。Phase 1。在完整细胞中,PF-03814735对Aurora1和Aurora2激酶的抑制活性降低磷酸-Aurora1 (Thr 232,Aurora1活性的敏感指标,IC50 ~ 20 nM),磷酸化组蛋白H3 (IC50 ~ 50 nM),和磷酸-Aurora2 (IC50 ~150 nM)的水平。PF-03814735阻断细胞质分裂,从而抑制细胞增殖和多倍体多核细胞的形成。[1]一项最近的研究表明小细胞肺癌(SCLC)和,在较小程度上,结肠癌细胞系均对PF-03814735非常敏感。Myc基因家族和成视网膜细胞瘤通路成员的状态与PF-03814735的功效显著相关。[1]
推荐供应商
货号品牌产品名称规格包装、参考价格
P873219MACKLINPF-0381473599%560元/1mg;   咨询
储存:-20℃
状态:粉末
PZ0218Sigma-AldrichPF-03814735≥98% (HPLC)1117.23元/5 MG;   4464.28元/25 MG;   咨询

产品说明

生化/生理作用

PF-03814735 is a potent inhibitor of Aurora kinase A and B (IC50 = 5 and 0.8 nM, respectively). PF-03814735 inhibits proliferation of tumor cells in culture and in xenograft tumor models. The compound PF-03814735 blocks phosphorylation of Aurora B and Histone H3, and leads to the formation of polyploid cells in culture (HCT116 and MDA-MB-231).

其他说明

This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

基本信息

经验(实验)分子式C23H25F3N6O2
分子量474.48
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
manufacturer/tradenamePfizer®
颜色 white to beige
溶解性DMSO: 20 mg/mL, clear
创始人Pfizer
储存温度−20℃

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
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