Flavopiridol (L86-8275)

Catalog No.S1230 Synonyms: NSC 649890 HCl, HMR-1275, Alvocidib

For research use only.

Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.

Flavopiridol (L86-8275) Chemical Structure

CAS No. 146426-40-6

Selleck's Flavopiridol (L86-8275) has been cited by 87 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

Other CDK Products

Biological Activity

Description Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Features First CDK inhibitor to be used in human clinical trials.
Targets
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)
Click to View More Targets
20 nM 30 nM 20-40 nM 40 nM 60 nM
In vitro

Flavopiridol displays less activity against unrelated kinases such as MAP, PAK, PKC, and EGFR with IC50 of >14 μM. Flavopiridol significantly inhibits the colony growth of HCT116, A2780, PC3, and Mia PaCa-2 cells with IC50 of 13 nM, 15 nM, 10 nM and 36 nM, respecitively. [1] Flavopiridol also potently inhibits the activity of Glycogen synthase kinase-3 (GSK-3) with an IC50 of 280 nm. [2] Compared with other CDKs, Flavopiridol inhibits the activity of CDK7 less potently with IC50 of 875 nM. Flavopiridol (0.5 μM) inhibits both pSer807/811 Rb and pThr199 NPM, whereas mild changes are observed at pThr821 Rb. Flavopiridol also decreases the overall RNA polymerase II level, as well as the phosphorylation of RNA polymerase II on the CTD repeats at Ser2 Ser5. [3] As a broad spectrum CDK inhibitor, Flavopiridol can inhibit cell cycle progression in either G1 or G2. Flavopiridol (0.3 μM) induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. [4] Flavopiridol exhibits potent cytotoxicity against a wide variety of tumor cell lines with IC50 values ranging form 16 nM for LNCAP to 130 nM for K562. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 tumor cell M4WySHBzd2yrZnXyZZRqd25iYYPzZZk> MmLQTY5pcWKrdHnvckBw\iCPQ1[tO{B1fW2xcjDj[YxtKHC{b3zp[oVz[XSrb36= NWP0UlNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC4OFMzOTFpPkGwPFQ{OjFzPD;hQi=>
PC3 cell M{fXOmZ2dmO2aX;uJIF{e2G7 M2TZXGlvcGmkaYTpc44hd2ZiUFOzJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0yOCEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTB4M{[wPUc,OTFyNkO2NFk9N2F-
HCT116 cell MlLlSpVv[3Srb36gZZN{[Xl? MmnYTY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> Mo\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTFyNkO2NFkoRjFzME[zOlA6RC:jPh?=
A2780 cell NGWxXFRHfW6ldHnvckBie3OjeR?= NV7qN29yUW6qaXLpeIlwdiCxZjDBNlc5OCClZXzsJINtd26xZ3XubYMh[XO|YYpvwKwhUUN3ME2xOUDPxE1? NF\FWZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC2N|YxQSd-MUGwOlM3ODl:L3G+
Mia PaCa-2 cell NXrFNZJyTnWwY4Tpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKE2rYTDQZWNiNTJiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUO2JO69VQ>? MnvkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTFyNkO2NFkoRjFzME[zOlA6RC:jPh?=
LNCaP human prostate carcinoma cell NEfr[JFRem:uaX\ldoF1cW:wIHHzd4F6 M4TrcGlvcGmkaYTpc44hd2ZiTF7DZXAhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvci=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
HCT116/VP35 human colon carcinoma cell MmnDVJJwdGmoZYLheIlwdiCjc4PhfS=> NFniNW5KdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= NIKyflk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
HCT116 human colon carcinoma cell MkjmVJJwdGmoZYLheIlwdiCjc4PhfS=> MlqwTY5pcWKrdHnvckBw\iCKQ2SxNVYhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1zODDuUS=> NUPMVVVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
HCT116/VM46 human colon carcinoma cell MlfRVJJwdGmoZYLheIlwdiCjc4PhfS=> M4HjbGlvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A2780/DDP-R human ovarian carcinoma cell MnHIVJJwdGmoZYLheIlwdiCjc4PhfS=> MnyyTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Ozhibl2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
ABAE human fibroblast cell NXTDblJCWHKxbHnm[ZJifGmxbjDhd5NigQ>? NV3HdJZJUW6qaXLpeIlwdiCxZjDBRmFGKGi3bXHuJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVQ2KG6P M3i0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
HL60 human leukemia cell MmPGVJJwdGmoZYLheIlwdiCjc4PhfS=> NEjiZnFKdmirYnn0bY9vKG:oIFjMOlAhcHWvYX6gcIV2c2WvaXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUS2JI5O M{\LOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
Hs 27 human fibroblast cell MkDqVJJwdGmoZYLheIlwdiCjc4PhfS=> M3TMSmlvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
CCRF-CEM human leukemia cell MVrQdo9tcW[ncnH0bY9vKGG|c3H5 M3W4WGlvcGmkaYTpc44hd2ZiQ1PSSk1ETU1iaIXtZY4hdGW3a3XtbYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVUzKG6P M4HtRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
OVCAR-3 human ovarian carcinoma cell NV7Ib3FzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKE:YQ1HSMVMhcHWvYX6gc5ZiemmjbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUW0JI5O Mkm1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
A2780/DDP-S human ovarian carcinoma cell M1vq[XBzd2yrZnXyZZRqd25iYYPzZZk> NIPPOnRKdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3TJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD13NjDuUS=> M2nxUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A2780/TAX-S human ovarian carcinoma cell NFG4cWNRem:uaX\ldoF1cW:wIHHzd4F6 MVfJcohq[mm2aX;uJI9nKEF{N{iwM3RCYC2VIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF03PSCwTR?= NILveFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
LS174T human colon carcinoma cell M1jwPHBzd2yrZnXyZZRqd25iYYPzZZk> Ml3iTY5pcWKrdHnvckBw\iCOU{G3OHQhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NTDuUS=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
MCF-7 human breast carcinoma cell NGizU2lRem:uaX\ldoF1cW:wIHHzd4F6 Ml7jTY5pcWKrdHnvckBw\iCPQ1[tO{BpfW2jbjDidoVie3RiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NjDuUS=> NF\FUVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
PC3 human prostate carcinoma cell M332PXBzd2yrZnXyZZRqd25iYYPzZZk> MVfJcohq[mm2aX;uJI9nKFCFMzDoeY1idiCycn;zeIF1\SClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
MLF mouse lung fibroblast cell Mmn4VJJwdGmoZYLheIlwdiCjc4PhfS=> NXnWVGluUW6qaXLpeIlwdiCxZjDNUGYhdW:3c3WgcJVv\yCoaXLyc4Jt[XO2IHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15MjDuUS=> MnnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
LX-1 human lung carcinoma M{L5ZXBzd2yrZnXyZZRqd25iYYPzZZk> NY\1VHJ4UW6qaXLpeIlwdiCxZjDMXE0yKGi3bXHuJIx2dmdiY3HyZ4lvd22jIIDyc4xq\mW{YYTpc44tKEmFNUC9O|Uhdk1? NXTldHNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
A431 human squamous cell NGfkdG1Rem:uaX\ldoF1cW:wIHHzd4F6 MU\Jcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P NX\Ve2RzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
SKBR-3 human breast carcinoma cell MXjQdo9tcW[ncnH0bY9vKGG|c3H5 MYjJcohq[mm2aX;uJI9nKFONQmKtN{BpfW2jbjDidoVie3RiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15NzDuUS=> M{LXdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A2780/TAX-R human ovarian carcinoma cell NXLzb|BPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHfxSWNKdmirYnn0bY9vKG:oIFGyO|gxN1SDWD3SJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15ODDuUS=> M4job|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
M109 mouse lung carcinoma cell M{fp[XBzd2yrZnXyZZRqd25iYYPzZZk> MXPJcohq[mm2aX;uJI9nKE1zMEmgcY92e2VibIXu[{Bk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVgxKG6P M3X5ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
CACO-2 human colon carcinoma cell NFPwVotRem:uaX\ldoF1cW:wIHHzd4F6 NUfZcmJxUW6qaXLpeIlwdiCxZjDDRWNQNTJiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME24OkBvVQ>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A549 human lung carcinoma cell MYTQdo9tcW[ncnH0bY9vKGG|c3H5 M3HTO2lvcGmkaYTpc44hd2ZiQUW0PUBpfW2jbjDseY5oKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:QTZibl2= MoDoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
MIP human colon carcinoma cell M{e0U2Z2dmO2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKE2LUDDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDsbY5mNCCLQ{WwQVAvOTJizszN NW[2T5BrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
K562 human leukemia cell NF7ZSWVRem:uaX\ldoF1cW:wIHHzd4F6 NWLPNnRrUW6qaXLpeIlwdiCxZjDLOVYzKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlE{KM7:TR?= M3i4TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
human A2780 cell line M2OzXnBzd2yrZnXyZZRqd25iYYPzZZk> M4SwV|czKGh? M1\4O2FvfGmycn;sbYZmemG2aY\lJIVn\mWldDDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGxibHnu[UB4[XNiZHX0[ZJucW6nZDDpckBiKHeqb3zlJINmdGxiN{KgbJIh[3m2b4TvfIlkcXS7IHHzd4F6NCCLQ{WwQVcyKG6P NWHsT3FJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwNlc5PjNpPkG1NFI4QDZ|PD;hQi=>
human ovarian (A2780) cancer cell Mo[3R5l1d3SxeHnjxsBie3OjeR?= M4S4fmN6fG:2b4jpZ{Bm\m[nY4Sgc44hcHWvYX6gc5ZiemmjbjCoRVI4QDBrIHPhcoNmeiClZXzsJIxqdmVuIFnDOVA:PzFibl2= NXu2VZB5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxNlU6PzFpPkG1NVI2QTdzPD;hQi=>
ID8 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 MmPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDJSFgh[2WubIOsJGlEPTB;NzDuUS=> NFzOWWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyN|gzOSd-MUexNlM5OjF:L3G+
MCF7 cells MoHuVJJwdGmoZYLheIlwdiCjc4PhfS=> NHLqPWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JG1ETjdiY3XscJMtKEmFNUC9NlYhdk1? MlTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzMkO4NlEoRjF5MUKzPFIyRC:jPh?=
Sf9 cells MWnGeY5kfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHP5Z4xqdiCDL1PET|Ih\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1zMjDuUS=> NGriTWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{mwOFM3Pid-MUe5NFQ{PjZ:L3G+
human A2780 cells NXjTfWtGTnWwY4Tpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGOmaz3t[YRq[XSnZDDOVG0heGixc4Doc5J6dGG2aX;uJIF1KHSqckG5PUBqdiCqdX3hckBCOjd6MDDj[Yxtew>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR4OUiwPUc,OTh2Nkm4NFk9N2F-
human A2780 cells MUHGeY5kfGmxbjDhd5NigQ>? MlvWNlQhcA>? M1npOWlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCC2aIK4NlEhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILz M4nUOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NE[5PFA6Lz5zOES2PVgxQTxxYU6=
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human NCI60 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 NY\Ibo1qPzJiaB?= MmXHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1m2NEBk\WyuczDhd5Nme3OnZDDhd{Bt\XSqYXyg[YZn\WO2IHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBNSzVyPUCuPVA1KM7:TR?= NX[zOHBnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwPFA4ODNpPkKxNFgxPzB|PD;hQi=>
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human MRC5 cells M{PNVmN6fG:2b4jpZ:Kh[XO|YYm= NICyVlY4OiCq NEWyeHhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlghdk1? NVOxTJB3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4PjdpPkKzN|AyPzZ5PD;hQi=>
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KB M1fDWWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXqzJIRigXN? NWDSd4t4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDh[pRmeiB|IHThfZMh[nliU2LCJI1mfGixZDygS2k2OCB;IECuNVYh|ryPLh?= M{L1U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG0PFA1Lz5{NUmxOFgxPDxxYU6=
KBVIN MULBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYezJIRigXN? M1XCSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1LWTW4h[2WubIOgZYZ1\XJiMzDkZZl{KGK7IGPSRkBu\XSqb3SsJGdKPTBiPTCwMlE5KM7:TT6= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzNEiwOEc,OjV7MUS4NFQ9N2F-
HCT116 Ml\5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4i3[|czKGi{cx?= M4HyXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtfGm2ZYKtS4xwKHKnYXflcpQh[mG|ZXSgZZN{[XliaX6gdJJme2WwY3Wgc4YhOTBnIH\leIFtKGKxdnnu[UB{\XK3bTygSWM2OCB;IECuNFM1KM7:TT6= NIfpSpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm4OVMxPSd-Mk[5PFU{ODV:L3G+
HCT116 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MnLOO|IhcHK| MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscJRqfGW{LVfsc{Bz\WGpZX70JIJie2WmIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJFAvPjJ3JTDm[ZRidCCkb4\pcoUhe2W{dX2sJGVEPTBiPTCwMlA2QSEQvF2u M4\JbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUi1N|A2Lz5{Nkm4OVMxPTxxYU6=
Sf9 MUnGeY5kfGmxbjDhd5NigQ>? MV:xNEBucW6| M2PGR2lvcGmkaYTpc44hd2ZiaIXtZY4hUGm|Nj30ZYdo\WRiQ1TLPU9kgWOuaX6gWFEh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnQSClZXzsd{B2e2mwZzDHV3QuS1SGIHHzJJN2[nO2cnH0[UBi\nSncjCxNEBucW6|IHnuJJBz\XOnbnPlJI9nKFupYX3tZU0{OlCfQWTQJIJ6KFOGUz3QRWdGKGGwYXz5d4l{NCCLQ{WwJF0hOC5yMEK1JO69VS5? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Sf21 NHvXbIlHfW6ldHnvckBie3OjeR?= NWLTPG4zUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBENXSncn3pcoFtKEirc{[teIFo\2WmIFPET|kw[3mlbHnuJHQyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDQSGt1cWSnIHHzJJN2[nO2cnH0[UwhUUN3MDC9JFAvODFzIN88UU4> NVLzV|dPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
HeLa NYXHU|RvS3m2b4TvfIlkcXS7IHHzd4F6 Ml\FO|IhcHK| NXK2V3k1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDDR|UxKD1iMD6xNkDPxE1w MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
sf21 MkHFSpVv[3Srb36gZZN{[Xl? NY\Rb49sUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEOGS{[vUk11\XKvaX7hcEBIW1RvdHHn[4VlKGO7Y3zpckBFOyCneIDy[ZN{\WRiaX6gd4YzOSClZXzsd{B2e2mwZzDobZN1d26nIFixJJN2[nO2cnH0[UwhUUN3MDC9JFAvOzl3IN88UU4> NHPm[pI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Sf21 NXfOO3g{TnWwY4Tpc44h[XO|YYm= M{j3ZWlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigR{11\XKvaX7hcEBJcXN4LYTh[4dm\CCFRFu3M4N6[2yrbjDIM24ufGW{bXnuZYwhT1OWLYTh[4dm\CCPQWSxJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lIyKGmwc3XjeEBk\WyuczD1d4lv\yClZHu3JJN2[nO2cnH0[UBx\XC2aXTlMEBKSzVyIE2gNE42OTRizszNMi=> M3S2U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
HepG2 NUmyW3lGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnvqO|IhcHK| M2izemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcHRqfGW{LVfsc{Bie3OjeTygSWM2OCB;IECuNVQ3PCEQvF2u MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
KOPN8 MnHyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGrrPIE4OiCqcoO= NVnPeldiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLU3BPQCClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtXGm2ZYKtS4xwKGG|c3H5MEBGSzVyIE2gNE4yQTJ4IN88UU4> M3LBTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO|k4PTxxYU6=
SEM NF3jNZRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVe3NkBpenN? MkPSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRV2gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbGTpeIVzNUeubzDhd5NigSxiRVO1NEA:KDBwMkC0N{DPxE1w MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
UOCB1 NUfuPJBOSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkDVO|IhcHK| M1zaWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVV;DRlEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcHRqfGW{LVfsc{Bie3OjeTygSWM2OCB;IECuNlA5PCEQvF2u NV3RUWNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
KOPN8 MonuRZBweHSxc3nzJIF{e2G7 NULsRWF5OC53IIXN MWOzJJRwKDJ2IHjydy=> MYXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuRUF64JINmdGy|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDjcIVifmWmIGDBVnAhdGW4ZXygZZQhOC53IIXNJIFnfGW{IEOgeI8hOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NEmzUHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO|k4PSd-Mkm0NFc6PzV:L3G+
KOPN8 NEDQe|lCeG:ydH;zbZMh[XO|YYm= NFPNU|UxNjVidV2= NYLFZm45OSCqch?= NV;TO4RvUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLU3BPQCClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4Yh[2ynYY\l[EBRSVKSIHzleoVtKGG2IECuOUB2VSCycnWteJJm[XSnZDD3bZRpKE6DQzDmc5IhOSCqcjDhcoQhdWWjc4Xy[YQh[W[2ZYKgN{B1dyB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
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
In vivo Administration of Flavopiridol at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, resulting in %T/C value of 110, and active against the human A2780 ovarian carcinoma implanted sc in nude mice, producing 1.5 log cell kill (LCK). [5] Flavopiridol treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. [6] In the p21-intact Hct116 xenografts in nude mice, administration of CPT-11 (100 mg/kg) followed by Flavopiridol (3 mg/kg) 7 and 16 hours later significantly inhibits tumor regression by 86% and 82%, respectively, displaying >2 fold inhibition compared with CPT-11 alone by 40 %. The combination produces ~30% complete response rate (CR) in contrast to CPT-11 alone where no CR is found. [7]

Protocol (from reference)

Kinase Assay:

[1]

  • CDK kinase assay:

    For CDK1/cyclin B1 kinase assay, kinase reactions consist of 100 ng of baculovirus expressed GST-CDK1/cyclin B1 (human) complex, 1 μg histone HI, 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT). For CDK2/cyclin E kinase assay, kinase reactions consist of 5 ng of baculovirus expressed GST-CDK2/cyclin E (human) complex, 0.5 μg GST-RB fusion protein (amino acids 776-928 of retinoblastoma protein), 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT). For CDK4/cyclin D1 kinase assay, kinase reactions consist of 150 ng of baculovirus expressed GST-CDK4/cyclin D1 (human), 280 ng of Stag-cyclin D1, 0.5 μg GST-RB fusion protein (amino acids 776-928 of retinoblastoma protein), 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT). Reactions are incubated for 45 minutes for CDK1 and CDK2, or 1 hour for CDK4 at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration 15%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Flavopiridol is dissolved at 10 mM in dimethylformamide (DMF) and evaluated at six concentrations, each in triplicate. The final concentration of DMF in the assay = 2%. IC50 values are derived by nonlinear regression analysis and have a coefficient of variance = 16%. To assay Flavopiridol activity on CDK6, a filter-binding assay is established. The following are combined in the reaction mixture: 2 μL of CDK6 (0.7 mg/μL), 5 μL of histone H1 (6 mg/mL), 14 μL of kinase buffer (60 mM β-glycerophosphate, 30 mM p-nitrophenyl phosphate, 25 mM MOPS (pH 7.0), 5 mM EGTA, 15 mM MgCl2, 1 mM DTT, 0.1 mM Na-vanadate), 3 μL of increasing concentrations of Flavopiridol diluted in 50% DMSO, and 6 μL of 33P-ATP (1 mCi/mL) in nonradioactive ATP at 90 μM concentration (final concentration: 15 μM). The assay is initiated by the addition of 33P-ATP. The reaction is incubated for 20 minutes at 30°C. A 25 μL aliquot of the supernatant is then spotted onto Whatman P81 phosphocellulose paper. Filters are washed 5 times with 1% phosphoric acid solution. Wet filters are counted in the presence of 1 mL of scintillation fluid. Cdk9 activity is measured using 50 nM of recombinant Cdk9/cyclin T in 50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 3 μM Na3VO4, 150 μM RNA polymerase CDT peptide and 80 μM ATP. Cdk7 assay is performed in the same buffer using 37 nM of purified kinase in the presence of 200 μM ATP and 10 μM myelin binding protein as a substrate. The potency of Flavopiridol toward CDK9 and CDK7 is determined using either a strong anion exchanger (Dowex 1-X8 resin, formate form)-based assay or a scintillation proximity assay. IC50 values are calculated from the dose-response curves.

Cell Research:

[5]

  • Cell lines: MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562 cells and et al.
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Flavopiridol for 72 hours at which time the tetrazolium dye, MTS in combination with phenazine methosulfate, is added. After 3 hours, the absorbency is measured at 492 nm, which is proportional to the number of viable cells. The results are expressed as IC50 values. For cell Cycle analysis, cells are fixed in paraformaldehyde and ethanol, washed, resuspended in staining solution of TdT enzyme and FITC-dUTP, washed, stained with PI following RNase treatment, and then analyzed by flow cytometry.

  • (Only for Reference)
Animal Research:

[5]

  • Animal Models: Female Balb/c×DBA/2J F1 mice inoculated ip with P388 ascites leukemic cells, and Balb/c nu/nu nude mice subcutaneous implanted with A2780, Br-cycE, or A431 cells
  • Dosages: ~7.5 mg/kg/day
  • Administration: Injection i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 15 mg/mL
(37.32 mM)
Water Insoluble
Ethanol ''''8 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

2.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 401.84
Formula

C21H20ClNO5

CAS No. 146426-40-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03441555 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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