Flavopiridol (L86-8275)

目录号:S1230 别名: NSC 649890 HCl, HMR-1275, Alvocidib 中文名称:夫拉平度

仅限科研使用

Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) 与ATP竞争性抑制CDKs,包括CDK1CDK2CDK4CDK6CDK9IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。

Flavopiridol (L86-8275) Chemical Structure

CAS: 146426-40-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 810.81 现货
RMB 647.01 现货
RMB 1386.75 现货
RMB 4668.25 现货
大包装 有超大折扣

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客户使用Selleck生产的Flavopiridol (L86-8275)发表文献100篇:

产品安全说明书

CDK抑制剂选择性比较

相关CDK产品

生物活性

产品描述 Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) 与ATP竞争性抑制CDKs,包括CDK1CDK2CDK4CDK6CDK9IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。
特性 Flavopiridol是第一个应用于人临床实验的细胞周期蛋白依赖性激酶抑制剂。
靶点
CDK9 [8]
(Cell-free assay)
CDK1 [8]
(Cell-free assay)
CDK4 [9]
(Cell-free assay)
CDK2 [8]
(Cell-free assay)
CDK6 [9]
(Cell-free assay)
点击更多
20 nM 30 nM 20-40 nM 40 nM 60 nM
体外研究

作为CDK广谱抑制剂,Flavopiridol可以抑制细胞周期进展,使其停在G1期或G2期。0.3 μM Flavopiridol作用于MCF-7或MDA-MB-468细胞,通过抑制CDK4或CDK2激酶活性,而诱导细胞周期停在G1 期。[4] Flavopiridol 作用于无关激酶,如MAP, PAK, PKC, 和 EGFR,活性低很多,IC50 >14 μM。Flavopiridol 显著抑制HCT116, A2780, PC3, 和 Mia PaCa-2 细胞集落生长,IC50分别为 13 nM, 15 nM, 10 nM, 和 36 nM。[1] Flavopiridol作用于多种肿瘤细胞系,具有细胞毒性,IC50为作用于LNCAP 的 16 nM 到作用于 K562的130 nM。[5] Flavopiridol也有效抑制糖原合成激酶-3(GSK-3) 的活性,IC50为 280 nm。[2]与其他CDKs相比, Flavopiridol抑制CDK7活性时效果稍弱,IC50为875 nM。 Flavopiridol (0.5 μM) 抑制pSer807/811 Rb 和pThr199 NPM,而在pThr821 Rb上观察到轻微变化。Flavopiridol也降低全部RNA聚合酶 II 水平, 及 RNA聚合酶 II在 CTD重复序列在 Ser2 Ser5位点磷酸化。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 tumor cell MXfQdo9tcW[ncnH0bY9vKGG|c3H5 NUX6S29mUW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh2M{KxNUc,OTB6NEOyNVE9N2F-
PC3 cell MWTGeY5kfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKFCFMzDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9NVAh|ryP NHr3Nnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC2N|YxQSd-MUGwOlM3ODl:L3G+
HCT116 cell NWLv[HMyTnWwY4Tpc44h[XO|YYm= M2HLZWlvcGmkaYTpc44hd2ZiSFPUNVE3KGOnbHygZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OD1zMzFOwG0> NWjkWYd2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUGwOlM3ODlpPkGxNFY{PjB7PD;hQi=>
A2780 cell NV20RWNETnWwY4Tpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKEF{N{iwJINmdGxiY3zvco9o\W6rYzDhd5Nige,:jDDJR|UxRTF3IN88US=> NGjwdVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC2N|YxQSd-MUGwOlM3ODl:L3G+
Mia PaCa-2 cell MoTPSpVv[3Srb36gZZN{[Xl? M2C5fGlvcGmkaYTpc44hd2ZiTXnhJHBiS2FvMjDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9N|Yh|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTB4M{[wPUc,OTFyNkO2NFk9N2F-
LNCaP human prostate carcinoma cell M2fSd3Bzd2yrZnXyZZRqd25iYYPzZZk> MWTJcohq[mm2aX;uJI9nKEyQQ3HQJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36= M4HYZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
HCT116/VP35 human colon carcinoma cell NHz0TnRRem:uaX\ldoF1cW:wIHHzd4F6 NH6wS4FKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= M2HqO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
HCT116 human colon carcinoma cell M2\I[HBzd2yrZnXyZZRqd25iYYPzZZk> NVi2XJNuUW6qaXLpeIlwdiCxZjDIR3QyOTZiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2xPEBvVQ>? NHPKSnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
HCT116/VM46 human colon carcinoma cell MXLQdo9tcW[ncnH0bY9vKGG|c3H5 M4f2ZWlvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= NG[1OpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
A2780/DDP-R human ovarian carcinoma cell NIniUWZRem:uaX\ldoF1cW:wIHHzd4F6 MUfJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0{QCCwTR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
ABAE human fibroblast cell NUO2XphYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHHzeZRKdmirYnn0bY9vKG:oIFHCRWUhcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OFUhdk1? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
HL60 human leukemia cell NX7WWGM5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2\yfGlvcGmkaYTpc44hd2ZiSFy2NEBpfW2jbjDs[ZVs\W2rYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NE[gcm0> NELXV4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
Hs 27 human fibroblast cell MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MonITY5pcWKrdHnvckBw\iCKczCyO{BpfW2jbjDmbYJzd2KuYYP0JINmdGxicILvcIln\XKjdHnvckwhUUN3ME21NUBvVQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
CCRF-CEM human leukemia cell MlHMVJJwdGmoZYLheIlwdiCjc4PhfS=> NEjvW5VKdmirYnn0bY9vKG:oIFPDVmYuS0WPIHj1cYFvKGyndXvlcYliKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OiCwTR?= Ml\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
OVCAR-3 human ovarian carcinoma cell M4DGSHBzd2yrZnXyZZRqd25iYYPzZZk> MnHXTY5pcWKrdHnvckBw\iCRVlPBVk0{KGi3bXHuJI93[XKrYX6gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21OEBvVQ>? NGWxUXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
A2780/DDP-S human ovarian carcinoma cell MnW1VJJwdGmoZYLheIlwdiCjc4PhfS=> NVLzTZNNUW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtV{BpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NU[gcm0> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A2780/TAX-S human ovarian carcinoma cell NH30PIJRem:uaX\ldoF1cW:wIHHzd4F6 NXnvUoZsUW6qaXLpeIlwdiCxZjDBNlc5OC:WQWitV{BpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NkWgcm0> NEn0dFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
LS174T human colon carcinoma cell NUi4fYZSWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnXRTY5pcWKrdHnvckBw\iCOU{G3OHQhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NTDuUS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
MCF-7 human breast carcinoma cell NYDmPIJ2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHTj[3hKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
PC3 human prostate carcinoma cell NFvvelJRem:uaX\ldoF1cW:wIHHzd4F6 M2[2S2lvcGmkaYTpc44hd2ZiUFOzJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;Nk[gcm0> MmKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
MLF mouse lung fibroblast cell NXLxZVY{WHKxbHnm[ZJifGmxbjDhd5NigQ>? M1TJ[GlvcGmkaYTpc44hd2ZiTVzGJI1wfXOnIHz1coch\mmkcn;icIF{fCClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PzJibl2= M4\1PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
LX-1 human lung carcinoma NH7hV5FRem:uaX\ldoF1cW:wIHHzd4F6 MYjJcohq[mm2aX;uJI9nKEy[LUGgbJVu[W5ibIXu[{Bk[XKlaX7vcYEheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> MlzHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
A431 human squamous cell MoHUVJJwdGmoZYLheIlwdiCjc4PhfS=> NUW5ZYtrUW6qaXLpeIlwdiCxZjDBOFMyKGi3bXHuJJNyfWGvb4XzJINmdGxiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> NH\UdYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
SKBR-3 human breast carcinoma cell MlS2VJJwdGmoZYLheIlwdiCjc4PhfS=> MVjJcohq[mm2aX;uJI9nKFONQmKtN{BpfW2jbjDidoVie3RiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15NzDuUS=> NUfnZpFURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
A2780/TAX-R human ovarian carcinoma cell MlztVJJwdGmoZYLheIlwdiCjc4PhfS=> NWHtTXQ2UW6qaXLpeIlwdiCxZjDBNlc5OC:WQWitVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;N{igcm0> NFX2XZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
M109 mouse lung carcinoma cell M1K0dHBzd2yrZnXyZZRqd25iYYPzZZk> NXvMdGF4UW6qaXLpeIlwdiCxZjDNNVA6KG2xdYPlJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16MDDuUS=> NW\DPZBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
CACO-2 human colon carcinoma cell M3TGVXBzd2yrZnXyZZRqd25iYYPzZZk> M2njemlvcGmkaYTpc44hd2ZiQ1HDU{0zKGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;OE[gcm0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A549 human lung carcinoma cell MYTQdo9tcW[ncnH0bY9vKGG|c3H5 MYnJcohq[mm2aX;uJI9nKEF3NEmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVk3KG6P NXrRcGl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
MIP human colon carcinoma cell Mmn4SpVv[3Srb36gZZN{[Xl? NH7ETWxKdmirYnn0bY9vKG:oIF3JVEBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBtcW6nLDDJR|UxRTBwMUKg{txO MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
K562 human leukemia cell MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 MXfJcohq[mm2aX;uJI9nKEt3NkKgbJVu[W5ibHX1b4VucWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTBwMUOg{txO Mmq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
human A2780 cell line MlvsVJJwdGmoZYLheIlwdiCjc4PhfS=> MVG3NkBp MVrBcpRqeHKxbHnm[ZJifGm4ZTDl[oZm[3RiYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxtKGyrbnWge4F{KGSndHXycYlv\WRiaX6gZUB4cG:uZTDj[YxtKDd{IHjyJIN6fG:2b4jpZ4l1gSCjc4PhfUwhUUN3ME23NUBvVQ>? NVvtem5TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwNlc5PjNpPkG1NFI4QDZ|PD;hQi=>
human ovarian (A2780) cancer cell NXfISmt{S3m2b4TvfIlkyqCjc4PhfS=> M2XBRmN6fG:2b4jpZ{Bm\m[nY4Sgc44hcHWvYX6gc5ZiemmjbjCoRVI4QDBrIHPhcoNmeiClZXzsJIxqdmVuIFnDOVA:PzFibl2= NH7wfHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUGyOVk4OSd-MUWxNlU6PzF:L3G+
ID8 cells M2LSdnBzd2yrZnXyZZRqd25iYYPzZZk> Mn;6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDJSFgh[2WubIOsJGlEPTB;NzDuUS=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF{M{iyNUc,OTdzMkO4NlE9N2F-
MCF7 cells MlPNVJJwdGmoZYLheIlwdiCjc4PhfS=> MkOwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNR2Y4KGOnbHzzMEBKSzVyPUK2JI5O MmDCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzMkO4NlEoRjF5MUKzPFIyRC:jPh?=
Sf9 cells Mmq2SpVv[3Srb36gZZN{[Xl? M{DhOWlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgZ5lkdGmwIFGvR2RMOiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUGyJI5O MkK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7MESzOlYoRjF5OUC0N|Y3RC:jPh?=
human A2780 cells NXzFcohZTnWwY4Tpc44h[XO|YYm= MVXJcohq[mm2aX;uJI9nKGOmaz3t[YRq[XSnZDDOVG0heGixc4Doc5J6dGG2aX;uJIF1KHSqckG5PUBqdiCqdX3hckBCOjd6MDDj[Yxtew>? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR4OUiwPUc,OTh2Nkm4NFk9N2F-
human A2780 cells M1rSOGZ2dmO2aX;uJIF{e2G7 NUTsT5hlOjRiaB?= M360UmlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCC2aIK4NlEhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILz M3TZXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NE[5PFA6Lz5zOES2PVgxQTxxYU6=
human NCI60 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 NVm5dY8{PzJiaB?= M2DiemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9O|QvPyCwTR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTB6MEewN{c,OjFyOEC3NFM9N2F-
human NCI60 cells NETZdoxRem:uaX\ldoF1cW:wIHHzd4F6 NVnpSoxoPzJiaB?= NUPwc291SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bie3Onc4Pl[EBieyCuZYToZYwh\W[oZXP0JIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCOQ{WwQVAvQTB2IN88US=> NHzpNGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUC4NFcxOyd-MkGwPFA4ODN:L3G+
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human A2780 cells MnO1R5l1d3SxeHnjxsBie3OjeR?= NXTpTXFWPzJiaB?= NGnhVppEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVI6KG6P NFfiOpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVc3Pyd-MkOzNFE4Pjd:L3G+
human A2780 cells NWPQN2ZVS3m2b4TvfIlkyqCjc4PhfS=> M2CzOFQ5KGh? MlPuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zNUBvVQ>? NFjxSpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVc3Pyd-MkOzNFE4Pjd:L3G+
human MRC5 cells NYXqcZpYS3m2b4TvfIlkyqCjc4PhfS=> Mo[wOFghcA>? MmXBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUO5JI5O M3rpXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|Y4Lz5{M{OwNVc3PzxxYU6=
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human HMEC1 cells MkexR5l1d3SxeHnjxsBie3OjeR?= NH64SlQ1QCCq NFvFcJdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYzKG6P NIq5TG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVc3Pyd-MkOzNFE4Pjd:L3G+
human HMEC1 cells MXPDfZRwfG:6aXRCpIF{e2G7 M1rJcVczKGh? Mn;DR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTG1GSzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME22OkBvVQ>? NGHRcpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVc3Pyd-MkOzNFE4Pjd:L3G+
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A2780 M{LIfWZ2dmO2aX;uJIF{e2G7 NELLbmE{OzBibl2= NUTiW4JLOjRiaIK= MW\Q[ZJk\W62YXflJGEzPzhyIHPlcIx{KGmwIGOtdIhie2ViYX\0[ZIhOjRiaIKgdkBifCB|M{Cgcm0hMEmFNUCpMEBE\WyuIHP5Z4xmKD1iMD6wNVYh|ryPLh?= Mn\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
A2780 M4PaSGZ2dmO2aX;uJIF{e2G7 NVT0Xo16OzNyIH7N NUPDTJE5OjRiaIK= MlHwVIVz[2WwdHHn[UBCOjd6MDDj[YxteyCrbjDHNk9OKGGodHXyJFI1KGi{IIKgZZQhOzNyIH7NJEhKSzVyKTygR4VtdCCleXPs[UA:KDBwMEKzJO69VS5? NWXrUmd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
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Sf21 MkTESpVv[3Srb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhS0SNOT;jfYNtcW5iVEGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmNlEhcW6|ZXP0JINmdGy|IIXzbY5oKFCGS4Tp[IUh[XNic4Xid5Rz[XSnLDDJR|UxKD1iMD6wNVEh|ryPLh?= NH62NZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
HeLa M4HVPGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{PH[FczKGi{cx?= MonER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCFQ{WwJF0hOC5zMjFOwG0v MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
sf21 MWrGeY5kfGmxbjDhd5NigQ>? NHu5b|BKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhS0SNNj;OMZRmem2rbnHsJGdUXC22YXfn[YQh[3mlbHnuJGQ{KGW6cILld5Nm\CCrbjDz[lIyKGOnbHzzJJV{cW6pIHjpd5RwdmViSEGgd5Vje3S{YYTlMEBKSzVyIE2gNE4{QTVizszNMi=> NUD4fFZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Sf21 MkDnSpVv[3Srb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhS0SNNz;jfYNtcW5iSD;OMZRmem2rbnHsJGdUXC22YXfn[YQhVUGWMTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[yNUBqdnOnY4SgZ4VtdHNidYPpcoch[2StNzDzeYJ{fHKjdHWgdIVxfGmmZTygTWM2OCB;IECuOVE1KM7:TT6= NYnPN3o2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
HepG2 MYjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1L4SVczKGi{cx?= MlzvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR|UxKD1iMD6xOFY1KM7:TT6= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
KOPN8 MnXNRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnjOO|IhcHK| MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuRUF64JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzUbZRmei2JbH:gZZN{[XluIFXDOVAhRSByLkG5NlYh|ryPLh?= NGfoW2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO|k4PSd-Mkm0NFc6PzV:L3G+
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KOPN8 NEXUbJZCeG:ydH;zbZMh[XO|YYm= NU\lVppKOC53IIXN MmfUNUBpeg>? NF\wPHJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKHC{ZT30doVifGWmIIfpeIghVkGFIH\vdkAyKGi{IHHu[EBu\WG|dYLl[EBi\nSncjCzJJRwKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NYe2WopiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
Assay
Methods Test Index PMID
Western blot Cleaved caspase-8 / Cleaved caspase-9 / Cleaved caspase-3 p-RNAPII / p-eIF4E / Mnk1 p-ERK / ERK / p-p38 / p-4EBP1 / 4EBP1 / p-S6 CDK2 / CDK4 / Cyclin A / p21 / p27 / Rb 31193061 24572052
Growth inhibition assay Cell viability 31193061
体内研究 Flavopiridol按7.5 mg/kg剂量处理P388 小鼠白血病,持续7天,具有轻微抗癌活性,导致%T/C值为110,且有效作用于皮下抑制人A2780卵巢癌的裸鼠,细胞对数杀灭(LCK)为1.5 。[5] Flavopiridol按 1-2.5 mg/kg 剂量处理小鼠,持续10天,通过抑制滑膜增生和关节损伤,而显著抑制胶原性关节炎,这种作用存在剂量依赖性,然而抗II型胶原(CII) 抗体的血清浓度,和II型胶原对应的增殖维持不变。[6]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1] [2] [3]

  • CDK 激酶实验:

    CDK1/cyclin B1 激酶实验中, 激酶反应包含100 ng表达 GST-CDK1/cyclin B1(人)复合体的 杆状病毒, 1 μg 组蛋白 HI, 0.2 μCi [γ-33P]ATP, 25 μM ATP溶于 50 μL 激酶buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT)。CDK2/cyclin E 激酶实验中, 激酶反应包含5 ng表达 GST-CDK2/cyclin E (人)复合体的杆状病毒, 0.5 μg GST-RB 融合蛋白(成视网膜细胞瘤蛋白776-928 氨基酸), 0.2 μCi [γ-33P]ATP, 25 μM ATP溶于 50 μL 激酶buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT)。CDK4/cyclin D1激酶实验中, 激酶反应含150 ng 表达GST-CDK4/cyclin D1 (人)的杆状病毒, 280 ng Stag-cyclin D1, 0.5 μg GST-RB 融合蛋白(成视网膜细胞瘤蛋白776-928 氨基酸), 0.2 μCi [γ-33P]ATP, 25 μM ATP 溶于50 μL激酶 buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT)。30oC下, CDK1 和CDK2反应温育45分钟, CDK4反应温育1小时,加入终浓度为15%的冰冻三氯乙酸(TCA) 终止反应。 使用Filtermate通用收集器,收集TCA沉淀物转移到GF/C 非过滤板上, 使用TopCount 96孔液体闪烁计数器测量过滤数。Flavopiridol溶于 10 mM二甲基甲酰胺(DMF) 中,测定六种浓度,每种重复测三次。实验中 DMF终浓度为 2%。通过回归曲线分析获得IC50值,变异系数为 16%。测定Flavopiridol作用于 CDK6的活性, 进行过滤-结合实验。 反应混合物按如下结合: 2 μL CDK6 (0.7 mg/μL), 5 μL 组蛋白 H1 (6 mg/mL), 14 μL 激酶 buffer (60 mM β-甘油磷酸, 30 mM p-磷酸硝基苯酯, 25 mM MOPS (pH 7.0), 5 mM EGTA, 15 mM MgCl2, 1 mM DTT, 0.1 mM 钒酸钠), 在50% DMSO中稀释的 3 μL 浓度不断增长的Flavopiridol ,及6 μL 33P-ATP (1 mCi/mL),非放射性 ATP,浓度为90 μM,(终浓度为15 μM)。加入33P-ATP开始反应。 反应在30oC下温育20分钟。25 μL等分的上清液点样到 Whatman P81 磷酸纤维素膜上。使用1% 磷酸溶液冲洗过滤器5次。 在1 mL闪烁液存在时测定湿过滤器。使用 50 nM 重组Cdk9/cyclin T在 50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 3 μM Na3VO4, 150 μM RNA 聚合酶CDT 肽和80 μM ATP中测定Cdk9活性。在相同buffer中使用37 nM纯化激酶,在200 μM ATP 存在时,10 μM 髓鞘蛋白(MBP)作为底物,进行Cdk7检测实验。使用强阴离子交换剂-为基础的检测实验或闪烁接近实验测定Flavopiridol 作用于CDK9和CDK7的效果。通过剂量反应曲线计算IC50值。

细胞实验:

[5]

  • Cell lines: MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562, 等等
  • Concentrations: 溶于DMSO,终浓度为 ~10 μM
  • Incubation Time: 72小时
  • Method:

    使用不同浓度 Flavopiridol 处理细胞72小时,加入四唑染料,MTS和吩嗪硫酸甲酯。3 小时后,在492 nm处测定吸光值,与存活细胞数成比例。结果表示为IC50值。为了分析细胞周期,细胞在仲甲醛和乙醇中混合,冲洗,然后再悬浮在TdT 酶和 FITC-dUTP染色液中,再冲洗,使用PI染色,随后进行RNA酶处理,最后使用流式细胞仪分析。

动物实验:

[5]

  • Animal Models: 腹腔注射P388 腹水白血病细胞的雌性Balb/c×DBA/2J F1小鼠,皮下移植A2780, Br-cycE, 或A431细胞的Balb/c nu/nu裸鼠
  • Dosages: ~7.5 mg/kg/day
  • Administration: 腹腔注射

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+ddH2O

2.5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 401.84
化学式

C21H20ClNO5

CAS号 146426-40-6
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03441555 Completed Drug: Venetoclax|Drug: Alvocidib Acute Myeloid Leukemia (AML) AbbVie|Sumitomo Pharma Oncology Inc. May 30 2018 Phase 1
NCT03298984 Completed Drug: Alvocidib|Drug: Cytarabine|Drug: Daunorubicin Acute Myeloid Leukemia Sumitomo Pharma Oncology Inc. September 25 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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