所有图片(1)
别名:
2-[(5-Hydroxy-1,5-dimethylhexyl)amino]-4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile hydrochloride
经验公式（希尔记法）:
C19H28N6O · HCl
推荐产品
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
CC1=CC(NC2=NNC(C)=C2)=NC(NC(C)CCCC(C)(C)O)=C1C#N.Cl
InChI
1S/C19H28N6O.ClH/c1-12-9-16(22-17-10-14(3)24-25-17)23-18(15(12)11-20)21-13(2)7-6-8-19(4,5)26;/h9-10,13,26H,6-8H2,1-5H3,(H3,21,22,23,24,25);1H
InChI key
DXVATYHPJJPMIN-UHFFFAOYSA-N
生化/生理作用
Orally active, potent and selective aurora A kinase inhibitor with anti-cancer activity in vitro and in vivo.
TC-A2317 (TC-A 2317) is an orally active, potent and selective aurora A kinase inhibitor (Ki = 1.2 nM; Aurora B Ki = 101 nM; IC50 >1 μM toward 60 other kinases). TC-A2317 inhibits the proliferation of human colorectal carcinoma HCT116 cells in cultures (IC50 = 115 nM) and suppresses HCT116 xenograft-derived tumor growth in mice in vivo (by 59% on day 14; 30 mg/kg/day p.o.) with good pharmacokinectic properties, oral bioavailability (Tmax = 1.2 h, T1/2 = 3.3 h, Cmax = 4930 nM, C60 min = 52 nM in rat serum post 30 mg/kg p.o.), and no adverse effects to the animals. TC-A231 is a racemate with its (S)-enantiomer being more active than the (R)-enantiomer (respective Ki = 0.59 vs. 66 nM).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Ryoichi Ando et al.
Bioorganic & medicinal chemistry letters, 20(15), 4709-4711 (2010-06-25)
A new class of Aurora A kinase inhibitor was created by transforming 4-(5-methyl-3-pyrazoloamino)pyrimidine moiety of VX-680 to 3-cyano-6-(5-methyl-3pyrazoloamino)pyridine. Compound 6 exhibited a potent Aurora A kinase inhibitory activity, excellent selectivity to Aurora B kinase and other 60 kinases, good cell
Cory T Zumbar et al.
Journal of neuro-oncology, 137(3), 481-492 (2018-02-06)
Glioblastoma is a highly malignant disease in critical need of expanded treatment options. The AURKA inhibitor alisertib exhibits antiproliferative activity against glioblastoma in vitro and in vivo. Unlike current clinically used taxane drugs, the novel taxane TPI 287 penetrates the
Weston Kenneth Ryan et al.
Cell death and differentiation, 26(3), 548-564 (2018-07-28)
The role of mitosis in the progression of precancerous skin remains poorly understood. To address this question, we deleted the mitotic Kinase Aurora-A (Aur-A) in hyperplastic mutant p53 mouse skin as an experimental tool to study the G2/M transition in
Yoo Hong Min et al.
Oncotarget, 7(51), 84718-84735 (2016-10-08)
Mitotic progression is crucial for the maintenance of chromosomal stability. A proper progression is ensured by the activities of multiple kinases. One of these enzymes, the serine/threonine kinase Aurora A, is required for proper mitosis through the regulation of centrosome
Arpan Kumar Rai et al.
Nature, 559(7713), 211-216 (2018-07-06)
Liquid-liquid phase separation has been shown to underlie the formation and disassembly of membraneless organelles in cells, but the cellular mechanisms that control this phenomenon are poorly understood. A prominent example of regulated and reversible segregation of liquid phases may
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