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1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-(942918-07-2)

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1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-エチル-1H-ピラゾール-3-イル]フェニル}-3,3-ジメチル尿素 製品概要
化学名:1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-エチル-1H-ピラゾール-3-イル]フェニル}-3,3-ジメチル尿素
英語化学名:GSK1070916
别名:N'-[4-[4-[2-[3-[(Dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl]phenyl]-N,N-dimethylurea;GSK1070916;3-(4-(4-(2-(3-((Dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea;N'-[4-[4-[2-[3-[(DiMethylaMino)Methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl;GSK-1070916A;GSK1070916;GSK 1070916;CS-364;GSK1070916;GSK-1070916;GSK 1070916
CAS番号:942918-07-2
分子式:C30H33N7O
分子量:507.63
EINECS:
カテゴリ情報:Inhibitors;Inhibitor
Mol File:942918-07-2.mol
1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-エチル-1H-ピラゾール-3-イル]フェニル}-3,3-ジメチル尿素
1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-エチル-1H-ピラゾール-3-イル]フェニル}-3,3-ジメチル尿素 物理性質
比重(密度) 1.21
貯蔵温度 Store at -20°C
溶解性≥25.4 mg/mL in DMSO
外見 solid
酸解離定数(Pka)13.17±0.40(Predicted)
安全性情報
MSDS Information
1-{4-[4-(2-{3-[(ジメチルアミノ)メチル]フェニル}-1H-ピロロ[2,3-b]ピリジン-4-イル)-1-エチル-1H-ピラゾール-3-イル]フェニル}-3,3-ジメチル尿素 Usage And Synthesis
使用GSK 1070916 is a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models.
定義ChEBI: 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-3-pyrazolyl]phenyl]-1,1-dimethylurea is a member of pyrazoles and a ring assembly.
生物活性gsk1070916 is a potent and selective inhibitor of aurora b/c kinase with ki values of 0.38nm and 1.5nm, respectively [1].gsk1070916 is a reversible atp-competitive inhibitor of aurora b and aurora c with ki values of 0.38nm and 1.5nm, respectively. the spa assay shows gsk1070916 has a good selectivity over aurora a. it inhibits aurora b with ic50 value of 5nm but 1259nm for aurora a. it is also reported that treatment of gsk1070916 suppresses cell proliferation in a549 human lung cancer cells with ec50 value of 7nm. moreover, both in vitro and in vivo assays demonstrate gsk1070916 can inhibit the phosphorylation of histone h3, which is a substrate of aurora b. gsk1070916 can also suppress tumor growth in mice with hl-60 tumor xenografts [1].
targetAurora B
参考文献[1] adams nd, adams jl, burgess jl, chaudhari am, copeland ra, donatelli ca, drewry dh, fisher ke, hamajima t, hardwicke ma, huffman wf, koretke-brown kk, lai zv, mcdonald ob, nakamura h, newlander ka, oleykowski ca, parrish ca, patrick dr, plant r, sarpong ma, sasaki k, schmidt sj, silva dj, sutton d, tang j, thompson cs, tummino pj, wang jc, xiang h, yang j, dhanak d. discovery of gsk1070916, a potent and selective inhibitor of aurora b/c kinase. j med chem. 2010 may 27;53(10):3973-4001.
Tags:942918-07-2