PF03814735 化学特性,用途語,生産方法
用途
Aurora kinases A 及びBに対する ATP 競合性阻害剤です（IC50 ＝ 0.8 nM（rAurora B），5
nM（rAurora A））。MDA-MB-231 細胞において、Aurora B, ヒストン H3, Aurora A のりん酸
化を阻害します（それぞれの IC50= 約 20 nM, 50 nM, 150 nM）。
用途
Aurora kinases A 及びBに対する ATP 競合性阻害剤です（IC50 ＝ 0.8 nmol/l（rAurora B），5
nmol/l（rAurora A））。MDA-MB-231 細胞において、Aurora B, ヒストン H3, Aurora A のりん
酸化を阻害します（それぞれの IC50= 約 20 nmol/l, 50 nmol/l, 150 nmol/l）。
説明
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-
03814735 is a reversible inhibitor of both Aurora A and B kinases with IC
50 values of 0.8 and 5 nM, respectively, in
in vitro activity assays. PF-
03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC
50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-
03814735 inhibits cell proliferation of HCT116, HL-
60, A549, and H125 tumor cell lines with IC
50 values ranging from 42-
150 nM and shows
in vivo efficacy in an HCT116 tumor xenograft mouse model. PF-
03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.
化学的特性
Off-White Solid
使用
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.[Cayman Chemical]
PF03814735 上流と下流の製品情報
原材料
準備製品