Flavopiridol (Alvocidib)

For research use only. Not for use in humans.

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

Flavopiridol (Alvocidib) Chemical Structure

CAS No. 146426-40-6

Flavopiridol (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。

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客户使用Selleck生产的Flavopiridol (Alvocidib)发表文献67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 (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)
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
ID8 cells NUW0VJFxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoXXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDJSFgh[2WubIOsJGlEPTB;NzDuUS=> NUXo[HpJOTdzMkO4NlE>
Sf9 cells MojoSpVv[3Srb36gZZN{[Xl? NVmwUoJ[UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBkgWOuaX6gRU9ETEt{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NVIhdk1? NXvBNnFXOTd7MESzOlY>
LNCaP human prostate carcinoma cell NYXkZ5Q6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MmH3TY5pcWKrdHnvckBw\iCOTlPhVEBpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;u MXyxNlE6ODNzMx?=
HCT116/VP35 human colon carcinoma cell NEnoPZhRem:uaX\ldoF1cW:wIHHzd4F6 NFPlO4lKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= MVyxNlE6ODNzMx?=
HCT116 human colon carcinoma cell MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MlvrTY5pcWKrdHnvckBw\iCKQ2SxNVYhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1zODDuUS=> M3fNUFEzOTlyM{Gz
HCT116/VM46 human colon carcinoma cell NET6PHVRem:uaX\ldoF1cW:wIHHzd4F6 M1LpeWlvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= NUPVXWJ6OTJzOUCzNVM>
human A2780 cells NVj0d5ljS3m2b4TvfIlkyqCjc4PhfS=> NHflOVgzPCCq MnvKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yN{BvVQ>? NV3hSIJCOjN|MEG3Olc>
MCF7 cells MmDHVJJwdGmoZYLheIlwdiCjc4PhfS=> M1HHXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWNHPyClZXzsd{whUUN3ME2yOkBvVQ>? MWixO|EzOzh{MR?=
human MRC5 cells M3vFO2N6fG:2b4jpZ:Kh[XO|YYm= NYPUToFWPzJiaB?= NX;QSlhiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVI5KG6P MVeyN|MxOTd4Nx?=
human A2780 cells MknpR5l1d3SxeHnjxsBie3OjeR?= MUG3NkBp M4m4fmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlkhdk1? M3m2PVI{OzBzN{[3
human A2780 cells M1nxdWN6fG:2b4jpZ:Kh[XO|YYm= NHqye2c1QCCq MlnqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zNUBvVQ>? NXXxS2JmOjN|MEG3Olc>
A2780/DDP-R human ovarian carcinoma cell MmLYVJJwdGmoZYLheIlwdiCjc4PhfS=> NYPheZdtUW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;M{igcm0> NX;oXGpCOTJzOUCzNVM>
human MRC5 cells Mn;lR5l1d3SxeHnjxsBie3OjeR?= MXG0PEBp M1nyemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zPUBvVQ>? M2H5eFI{OzBzN{[3
ABAE human fibroblast cell MUfQdo9tcW[ncnH0bY9vKGG|c3H5 M3H0NGlvcGmkaYTpc44hd2ZiQVLBSUBpfW2jbjDmbYJzd2KuYYP0JINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OUBvVQ>? MWWxNlE6ODNzMx?=
HL60 human leukemia cell NYrPWnpWWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml7TTY5pcWKrdHnvckBw\iCKTE[wJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD12NjDuUS=> Mn\ENVIyQTB|MUO=
human MRC5 cells M4LwdmN6fG:2b4jpZ:Kh[XO|YYm= NF:3SoMzPCCq NWnteJROS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVQ6KG6P NH23[4szOzNyMUe2Oy=>
Hs 27 human fibroblast cell NYKwN|VMWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mk[zTY5pcWKrdHnvckBw\iCKczCyO{BpfW2jbjDmbYJzd2KuYYP0JINmdGxicILvcIln\XKjdHnvckwhUUN3ME21NUBvVQ>? M{DDfFEzOTlyM{Gz
CCRF-CEM human leukemia cell NXmzNoE2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NX\Weo5iUW6qaXLpeIlwdiCxZjDDR3JHNUOHTTDoeY1idiCuZYXr[Y1q[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTJibl2= NIG3eXEyOjF7MEOxNy=>
OVCAR-3 human ovarian carcinoma cell MnfoVJJwdGmoZYLheIlwdiCjc4PhfS=> M2\WR2lvcGmkaYTpc44hd2ZiT2\DRXIuOyCqdX3hckBwfmG{aXHuJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVQhdk1? MYqxNlE6ODNzMx?=
A2780/DDP-S human ovarian carcinoma cell NGXofXlRem:uaX\ldoF1cW:wIHHzd4F6 NX\XOnU1UW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtV{BpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NU[gcm0> MlLBNVIyQTB|MUO=
human HMEC1 cells M4L1bWN6fG:2b4jpZ:Kh[XO|YYm= NF;pVowzPCCq NITLTJNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYyKG6P Mn\DNlM{ODF5Nke=
human HMEC1 cells MnewR5l1d3SxeHnjxsBie3OjeR?= NVLnW5E3PDhiaB?= M{fsSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhOTUNzIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEeLNUC9OlIhdk1? MnL6NlM{ODF5Nke=
A2780/TAX-S human ovarian carcinoma cell MnXsVJJwdGmoZYLheIlwdiCjc4PhfS=> MlPrTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PjVibl2= MUexNlE6ODNzMx?=
LS174T human colon carcinoma cell Mn7mVJJwdGmoZYLheIlwdiCjc4PhfS=> NYfINJpWUW6qaXLpeIlwdiCxZjDMV|E4PFRiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OUBvVQ>? NEDOfIMyOjF7MEOxNy=>
MCF-7 human breast carcinoma cell MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NF3We29KdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MVWxNlE6ODNzMx?=
human HMEC1 cells NXfUd3NvS3m2b4TvfIlkyqCjc4PhfS=> M{f2NVczKGh? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[2JI5O MojNNlM{ODF5Nke=
PC3 human prostate carcinoma cell Mm\CVJJwdGmoZYLheIlwdiCjc4PhfS=> NGPTUlBKdmirYnn0bY9vKG:oIGDDN{BpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MoD5NVIyQTB|MUO=
human A2780 cell line MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 MkO0O|IhcA>? MkSyRY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9O|Ehdk1? M1joeVE2ODJ5OE[z
human ovarian (A2780) cancer cell M1L0NGN6fG:2b4jpZ:Kh[XO|YYm= MVXDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P M323W|E2OTJ3OUex
MLF mouse lung fibroblast cell NYXST4lnWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVK0OnVsUW6qaXLpeIlwdiCxZjDNUGYhdW:3c3WgcJVv\yCoaXLyc4Jt[XO2IHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15MjDuUS=> MlzQNVIyQTB|MUO=
human NCI60 cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 MoTmO|IhcA>? MoW3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1m2NEBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME23OE44KG6P NH:xWYEzOTB6MEewNy=>
LX-1 human lung carcinoma MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NYDLO4g3UW6qaXLpeIlwdiCxZjDMXE0yKGi3bXHuJIx2dmdiY3HyZ4lvd22jIIDyc4xq\mW{YYTpc44tKEmFNUC9O|Uhdk1? NI[3e48yOjF7MEOxNy=>
A431 human squamous cell NVjMNYRxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH\a[pRKdmirYnn0bY9vKG:oIFG0N|EhcHWvYX6gd5F2[W2xdYOgZ4VtdCClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTd3IH7N Ml\kNVIyQTB|MUO=
SKBR-3 human breast carcinoma cell NHS2bZJRem:uaX\ldoF1cW:wIHHzd4F6 NYOxfVN4UW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? M2XxdFEzOTlyM{Gz
A2780/TAX-R human ovarian carcinoma cell MoTlVJJwdGmoZYLheIlwdiCjc4PhfS=> MYnJcohq[mm2aX;uJI9nKEF{N{iwM3RCYC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04QCCwTR?= MYGxNlE6ODNzMx?=
M109 mouse lung carcinoma cell M4TVT3Bzd2yrZnXyZZRqd25iYYPzZZk> NEDzPXJKdmirYnn0bY9vKG:oIF2xNFkhdW:3c3WgcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRThyIH7N M13wZlEzOTlyM{Gz
CACO-2 human colon carcinoma cell MnSyVJJwdGmoZYLheIlwdiCjc4PhfS=> MU\Jcohq[mm2aX;uJI9nKEODQ1:tNkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTh4IH7N NF3YRpkyOjF7MEOxNy=>
A549 human lung carcinoma cell MXHQdo9tcW[ncnH0bY9vKGG|c3H5 M1rtW2lvcGmkaYTpc44hd2ZiQUW0PUBpfW2jbjDseY5oKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:QTZibl2= Moq5NVIyQTB|MUO=
MIP human colon carcinoma cell MkixSpVv[3Srb36gZZN{[Xl? M2fmVWlvcGmkaYTpc44hd2ZiTVnQJIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJIxqdmVuIFnDOVA:OC5zMjFOwG0> NIXsNYQyOjF7MEOxNy=>
K562 human leukemia cell NXjncI9jWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mki2TY5pcWKrdHnvckBw\iCNNU[yJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1yLkGzJO69VQ>? M3[5UVEzOTlyM{Gz
MCF-7 tumor cell M4DuTHBzd2yrZnXyZZRqd25iYYPzZZk> NUXTNY55UW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> M2jpW|ExQDR|MkGx
human NCI60 cells NIXKeFRRem:uaX\ldoF1cW:wIHHzd4F6 NEHkTYo4OiCq M1vZWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZZN{\XO|ZXSgZZMhdGW2aHHsJIVn\mWldDDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhVEN3ME2wMlkxPCEQvF2= MXWyNVA5ODdyMx?=
PC3 cell NWPl[ox[TnWwY4Tpc44h[XO|YYm= M{jMdWlvcGmkaYTpc44hd2ZiUFOzJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0yOCEQvF2= M2LsdFEyODZ|NkC5
HCT116 cell NGTmUmtHfW6ldHnvckBie3OjeR?= MlvZTY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> NH\vc5gyOTB4M{[wPS=>
A2780 cell NHvoXlVHfW6ldHnvckBie3OjeR?= MnTsTY5pcWKrdHnvckBw\iCDMke4NEBk\WyuIHPsc45w\2WwaXOgZZN{[XoxvJygTWM2OD1zNTFOwG0> NIfDT2UyOTB4M{[wPS=>
Mia PaCa-2 cell MlyxSpVv[3Srb36gZZN{[Xl? NIr2NnVKdmirYnn0bY9vKG:oIF3pZUBR[UOjLUKgZ4VtdCClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVM3KM7:TR?= NWW3OotVOTFyNkO2NFk>
human A2780 cells M{iyb2Z2dmO2aX;uJIF{e2G7 NEn4bmdKdmirYnn0bY9vKG:oIHPkb{1u\WSrYYTl[EBPWE1icHjvd5Bpd3K7bHH0bY9vKGG2IITodlE6QSCrbjDoeY1idiCDMke4NEBk\Wyucx?= MmjMNVg1Pjl6MEm=
human A2780 cells MoSwSpVv[3Srb36gZZN{[Xl? M{XydVI1KGh? NHu3TIpKdmirYnn0bY9vKG:oIHPkb{1u\WSrYYTl[EBT[iCyaH;zdIhwenmuYYTpc44h[XRidHjyPFIyKGmwIHj1cYFvKEF{N{iwJINmdGy|IHHmeIVzKDJ2IHjydy=> NFT6RmcyQDR4OUiwPS=>

... 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-eIF4ES209 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-BP1Thr70) 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 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]

- 合并

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]

- 合并
  • 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。


    (Only for Reference)
动物实验:

[5]

- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 15 mg/mL (37.32 mM)
Ethanol 8 mg/mL (19.9 mM)
Water 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):
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 粉状
溶于溶剂
别名 NSC 649890 HCl,HMR-1275

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、MSDS / 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、MSDS / 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
NCT03441555 Active not recruiting Drug: Venetoclax|Drug: Alvocidib Acute Myeloid Leukemia (AML) AbbVie|Sumitomo Dainippon Pharma Oncology Inc May 30 2018 Phase 1
NCT03298984 Completed Drug: Alvocidib|Drug: Cytarabine|Drug: Daunorubicin Acute Myeloid Leukemia Sumitomo Dainippon Pharma Oncology Inc September 25 2017 Phase 1

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID