Flavopiridol (L86-8275) HCl

For research use only. Not for use in humans.

目录号:S2679 别名: NSC 649890, Alvocidib, HMR-1275, DSP-2033 中文名称:盐酸夫拉平度

Flavopiridol (L86-8275) HCl Chemical Structure

CAS No. 131740-09-5

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs,作用于CDK1CDK2CDK4CDK6,无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 819.17 现货
RMB 903.08 现货
RMB 1813.43 现货
RMB 3121.42 现货
RMB 5569.2 现货
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客户使用Selleck生产的Flavopiridol (L86-8275) HCl发表文献37篇:

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs,作用于CDK1CDK2CDK4CDK6,无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。
靶点
CDK1 [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
CDK7 [1]
(Cell-free assay)
40 nM 40 nM 40 nM 40 nM 300 nM
体外研究

Flavopiridol最初被发现抑制表皮生长因子受体和蛋白激酶A的活性,IC50分别是21 μM and 122 μM。Flavopiridol是后来证明能够抑制细胞的增殖,在多种生理相关浓度(IC50 = 66 nM),在肿瘤细胞系美国国家癌症研究所开发治疗计划中的60种人癌细胞系测试过。[1] Flavopiridol以时间和浓度依赖性方式诱导人类乳腺癌细胞G1期阻滞并抑制CDK2和CDK4。[2] Flavopiridol短时处理(约12小时)诱导造血细胞系的细胞凋亡,包括SUDHL4,SUDHL6(B细胞系),Jurkat和MOLT4(T细胞系)和HL60(髓细胞系)。[3] 在克隆形成实验中,Flavopiridol在23人肿瘤模型中表现高细胞毒性,平均IC70是8 ng/mL。[4] 最近的一项研究表明Flavopiridol诱导人脑胶质瘤T98G细胞系的AKT-Ser473磷酸化。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 tumor cell MkTMVJJwdGmoZYLheIlwdiCjc4PhfS=> MYPJcohq[mm2aX;uJI9nKE2FRj23JJR2dW:{IHPlcIwheHKxbHnm[ZJifGmxbh?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh2M{KxNUc,OTB6NEOyNVE9N2F-
Mia PaCa-2 cell NHLiem5HfW6ldHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKE2rYTDQZWNiNTJiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUO2JO69VQ>? NGHiW|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC2N|YxQSd-MUGwOlM3ODl:L3G+
A2780 cell M1HlNWZ2dmO2aX;uJIF{e2G7 NYHpcnM2UW6qaXLpeIlwdiCxZjDBNlc5OCClZXzsJINtd26xZ3XubYMh[XO|YYpvwKwhUUN3ME2xOUDPxE1? MkPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTFyNkO2NFkoRjFzME[zOlA6RC:jPh?=
HCT116 cell NEDISJZHfW6ldHnvckBie3OjeR?= NVrPbHJ2UW6qaXLpeIlwdiCxZjDIR3QyOTZiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUGzJO69VQ>? M{jSPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzME[zOlA6Lz5zMUC2N|YxQTxxYU6=
PC3 cell MkDESpVv[3Srb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKFCFMzDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9NVAh|ryP M4PWeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzME[zOlA6Lz5zMUC2N|YxQTxxYU6=
K562 human leukemia cell NF7JVnZRem:uaX\ldoF1cW:wIHHzd4F6 M{LyZ2lvcGmkaYTpc44hd2ZiS{W2NkBpfW2jbjDs[ZVs\W2rYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD6xN{DPxE1? M3TiRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
MIP human colon carcinoma cell M4\MOGZ2dmO2aX;uJIF{e2G7 MorPTY5pcWKrdHnvckBw\iCPSWCgbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygcIlv\SxiSVO1NF0xNjF{IN88US=> M4PjSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A549 human lung carcinoma cell MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NVTncHoxUW6qaXLpeIlwdiCxZjDBOVQ6KGi3bXHuJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD17NjDuUS=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
CACO-2 human colon carcinoma cell NV:xVFM5WHKxbHnm[ZJifGmxbjDhd5NigQ>? MonyTY5pcWKrdHnvckBw\iCFQVPPMVIhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16NjDuUS=> MkjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
M109 mouse lung carcinoma cell NYToTnpzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWjLUVI1UW6qaXLpeIlwdiCxZjDNNVA6KG2xdYPlJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16MDDuUS=> NWjkTJl3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
A2780/TAX-R human ovarian carcinoma cell Moq1VJJwdGmoZYLheIlwdiCjc4PhfS=> MYLJcohq[mm2aX;uJI9nKEF{N{iwM3RCYC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04QCCwTR?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
SKBR-3 human breast carcinoma cell MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 NVLQTWFIUW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? MoPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
A431 human squamous cell MmfrVJJwdGmoZYLheIlwdiCjc4PhfS=> MYrJcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P M3HTNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
LX-1 human lung carcinoma M4rPTnBzd2yrZnXyZZRqd25iYYPzZZk> MVPJcohq[mm2aX;uJI9nKEy[LUGgbJVu[W5ibIXu[{Bk[XKlaX7vcYEheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
MLF mouse lung fibroblast cell NGDaPZFRem:uaX\ldoF1cW:wIHHzd4F6 M2npcWlvcGmkaYTpc44hd2ZiTVzGJI1wfXOnIHz1coch\mmkcn;icIF{fCClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PzJibl2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
PC3 human prostate carcinoma cell NFjuRW1Rem:uaX\ldoF1cW:wIHHzd4F6 NFj0d3BKdmirYnn0bY9vKG:oIGDDN{BpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O NIL2fGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
MCF-7 human breast carcinoma cell NG[4UHBRem:uaX\ldoF1cW:wIHHzd4F6 NH7YdGNKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O M4XXb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
LS174T human colon carcinoma cell M{PtdHBzd2yrZnXyZZRqd25iYYPzZZk> NFnLSJJKdmirYnn0bY9vKG:oIFzTNVc1XCCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[1JI5O MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A2780/TAX-S human ovarian carcinoma cell NGrURnBRem:uaX\ldoF1cW:wIHHzd4F6 M2f1d2lvcGmkaYTpc44hd2ZiQUK3PFAwXEG[LWOgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ3IH7N MkHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
A2780/DDP-S human ovarian carcinoma cell MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MoTSTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTZibl2= M4TuO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
OVCAR-3 human ovarian carcinoma cell MlvoVJJwdGmoZYLheIlwdiCjc4PhfS=> MnrhTY5pcWKrdHnvckBw\iCRVlPBVk0{KGi3bXHuJI93[XKrYX6gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21OEBvVQ>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
CCRF-CEM human leukemia cell NFTDdXVRem:uaX\ldoF1cW:wIHHzd4F6 MXPJcohq[mm2aX;uJI9nKEOFUl[tR2VOKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21NkBvVQ>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
Hs 27 human fibroblast cell NFLlNJpRem:uaX\ldoF1cW:wIHHzd4F6 M2fwXmlvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? Mlf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
HL60 human leukemia cell MWjQdo9tcW[ncnH0bY9vKGG|c3H5 Ml\kTY5pcWKrdHnvckBw\iCKTE[wJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD12NjDuUS=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
ABAE human fibroblast cell MlXRVJJwdGmoZYLheIlwdiCjc4PhfS=> M1vPTWlvcGmkaYTpc44hd2ZiQVLBSUBpfW2jbjDmbYJzd2KuYYP0JINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OUBvVQ>? NY\D[VNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
A2780/DDP-R human ovarian carcinoma cell M3LLWHBzd2yrZnXyZZRqd25iYYPzZZk> NVfITJJnUW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;M{igcm0> M1Ozb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
HCT116/VM46 human colon carcinoma cell MoT0VJJwdGmoZYLheIlwdiCjc4PhfS=> NHSxVlZKdmirYnn0bY9vKG:oIFjDWFEyPi:YTUS2JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OjFibl2= NGDVUlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
HCT116 human colon carcinoma cell NGrHdZdRem:uaX\ldoF1cW:wIHHzd4F6 NWTwb3IzUW6qaXLpeIlwdiCxZjDIR3QyOTZiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2xPEBvVQ>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
HCT116/VP35 human colon carcinoma cell NF7keGRRem:uaX\ldoF1cW:wIHHzd4F6 NXzPdW1tUW6qaXLpeIlwdiCxZjDIR3QyOTZxVmCzOUBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTF5IH7N MmfzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
LNCaP human prostate carcinoma cell MXPQdo9tcW[ncnH0bY9vKGG|c3H5 M4rFUGlvcGmkaYTpc44hd2ZiTF7DZXAhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvci=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
human A2780 cell line M2rKZnBzd2yrZnXyZZRqd25iYYPzZZk> MoO2O|IhcA>? M13KbmFvfGmycn;sbYZmemG2aY\lJIVn\mWldDDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGxibHnu[UB4[XNiZHX0[ZJucW6nZDDpckBiKHeqb3zlJINmdGxiN{KgbJIh[3m2b4TvfIlkcXS7IHHzd4F6NCCLQ{WwQVcyKG6P MmjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyMke4OlMoRjF3MEK3PFY{RC:jPh?=
human ovarian (A2780) cancer cell MWXDfZRwfG:6aXRCpIF{e2G7 MXTDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF{NUm3NUc,OTVzMkW5O|E9N2F-
ID8 NF3lOG1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0 MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFnEPEBk\WyuczygTWM2OD1yLkCwO:69VQ>? M1v1[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUKzPFIyLz5zN{GyN|gzOTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved caspase-8 / Cleaved caspase-9 / Cleaved caspase-3; 

PubMed: 31193061     


(C) Caspase activation was determined by western blotting. Flavopiridol treatment (300 nM) induced the expressions of cleaved caspase-8, -9 and -3 in a time-dependent manner. 

p-RNAPII / p-eIF4E / Mnk1; 

PubMed: 24572052     


After 24 h drug exposure, CDKI-73 or flavopiridol also abolished p-eIF4E(S209) at 0.25 μM, indicating cellular inhibition of Mnk kinase activity. The same treatment with CDKI-73 or flavopiridol caused a loss in Mnk1 protein expression. CGP57380-treated cells abrogated p-RNAPIIS2 as well as p-eIF4E(S209) with a minimal effect on Mnk1 protein level.

p-ERK / ERK / p-p38 / p-4EBP1 / 4EBP1 / p-S6; 

PubMed: 24572052     


0.25 μM CDKI-73 or flavopiridol caused little changes in the phosphorylation of Erk and p38 MAPK; however, inhibited the 4E-BP1 phosphorylation [p-4E-BP1(Thr70)] by 24 h. CGP57380 had a minimal effect on these proteins.

CDK2 / CDK4 / Cyclin A / p21 / p27 / Rb; 

PubMed: 24572052     


Effect of flavopiridol on cell cycle-related protein expression in uterine leiomyoma cells. Twenty-four hours after treatment, cell extracts were prepared and subjected to immunoblotting analysis. β-Actin was used as an internal loading control.

31193061 24572052
Growth inhibition assay
Cell viability; 

PubMed: 31193061     


The antiproliferative effect of flavopiridol on CCA cell lines was determined using an MTT assay. KKU-055, KKU-100, KKU-213 and KKU-214 cells were treated with 50, 100, 200 or 300 nM of flavopiridol at 24, 48 or 72 h. The percentage of cell number in vehicle control was taken as 100%. Data are mean ± SD of three independent experiments. *P < 0.05 in all CCA cell lines, significantly different for each time point compared with vehicle control.

31193061
体内研究 以最大耐受剂量10 mg/kg/day在第1-4天及7-11天给药,Flavopiridol表现为PRXF1337肿瘤消退和PRXF1369肿瘤停滞为期4周。[4] 用7.5 mg/kg Flavopiridol静脉内(IV)或腹膜内连续注射5天后,12分之11的皮下(SC)人HL-60 移植鼠的肿瘤完全消退,Flavopiridol治疗一疗程后移植鼠数月无病。在SUDHL-4皮下注射淋巴瘤模型鼠中静脉注射Flavopiridol (7.5 mg/kg),模型鼠的肿瘤大部分(8分之2)或者完全(8分之4)消退,两只剩余动物无病超过60天。整体生长延迟73.2%。[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]
- 合并

重组CDKs激酶反应:

CDKs的活性按如下方式在酶标板中,40 μg GST-R b与不同量Flavopiridol和未标记的ATP混合。反应然后通过加入S100的馏分从表达重组人CDK的昆虫细胞中得到的硫酸铵沉淀部分的开始。最终反应条件为10 mM MgCl2, 50 mM Tris-HCl (pH 7.5)和1 mM DTT。ATP的终浓度做相应的调整。放射性标记的ATP作为磷酸供体。该反应在30℃下加入酶后进行2.5分钟,然后加入EDTA终止。GST-Rb用谷胱甘肽 - 琼脂糖标记和掺入的放射性通过液体闪烁计数测定。
细胞实验:[2]
- 合并
  • Cell lines: SUDHL4, SUDHL6, Jurkat, MOLT4和HL60细胞
  • Concentrations: 0, 100 500, 5000 nM
  • Incubation Time: 14小时
  • Method: 在密度为1 × 106 cells/mL的细胞中不同时间加入不同浓度的Flavopiridol。提取DNA。细胞用冷的磷酸盐缓冲盐水(PBS)洗涤一次并在4℃条件下在3 mL裂解缓冲液(5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100)中裂解15分钟。将细胞裂解物的染色质(以26,000 g,4℃,20分钟)离心分离。用苯酚,酚氯仿(1:1)和氯仿从上清液提取提取小的DNA片段。核酸在-20℃中在0.5M氯化钠,90%的乙醇沉淀过夜。RNA由牛RNAaseA消化(60μg/mL)。连续反萃取和沉淀后,DNA溶解在10mM Tris-HCl(pH值7.5),1mM的EDTA,0.5%十二烷基硫酸钠(SDS),而后在1.6%琼脂糖凝胶上电泳。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 人类前列腺癌异种移植,PRXFI337和PRXFI369,皮下种植在裸鼠中
  • Dosages: 10 mg/kg/d
  • Administration: 在days 1-4 and 7-11口服。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 88 mg/mL (200.77 mM)
Water Insoluble
Ethanol Insoluble
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):
2% DMSO+30% PEG 300+ddH2O
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 438.3
化学式

C21H20ClNO5.HCl

CAS号 131740-09-5
储存条件 粉状
溶于溶剂
别名 NSC 649890, Alvocidib, HMR-1275, DSP-2033

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00112723 Terminated Drug: alvocidib Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Multiple Myeloma|Splenic Marginal Zone Lymphoma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma|Waldenström Macroglobulinemia National Cancer Institute (NCI) December 2005 Phase 1|Phase 2
NCT00098371 Terminated Drug: alvocidib B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia National Cancer Institute (NCI) April 2005 Phase 2
NCT00101231 Terminated Drug: alvocidib Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia National Cancer Institute (NCI) October 2004 Phase 1
NCT00058240 Completed Drug: alvocidib B-cell Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Waldenström Macroglobulinemia National Cancer Institute (NCI) April 2003 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID