Flavopiridol (L86-8275) HCl

Catalog No.S2679 Synonyms: NSC 649890, Alvocidib, HMR-1275, DSP-2033

For research use only.

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.

Flavopiridol (L86-8275) HCl Chemical Structure

CAS No. 131740-09-5

Selleck's Flavopiridol (L86-8275) HCl has been cited by 44 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

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Biological Activity

Description Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Targets
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
In vitro

Flavopiridol is initially found to inhibit the epidermal growth factor receptor and protein kinase A (IC50 = 21 and 122 μM). Flavopiridol is later shown to inhibit cell proliferation, at more physiologically relevant concentrations (IC50 = 66 nM) when Flavopiridol is tested in the National Cancer Institute Development Therapeutics Program panel of 60 human tumor cell lines. [1] Flavopiridol induces G1 arrest with inhibition of CDK2 and CDK4 in human breast carcinoma cells in a time and concentration dependent manner. [2] Short time treatment of Flavopiridol (~12 hours) induce apoptosis in hematopoietic cell lines including SUDHL4, SUDHL6 (B-cell lines), Jurkat and MOLT4 (T-cell lines ), and HL60 (myeloid). [3] In the clonogenic assay, Flavopiridol functions as a highly potent cytotoxic compound with a mean IC70 with 8 ng/mL in 23 human tumor models. [4] A recent study shows Flavopiridol treatment induces a substantial AKT-Ser473 phosphorylation in human glioblastoma T98G cell line. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 tumor cell MUHQdo9tcW[ncnH0bY9vKGG|c3H5 MlnITY5pcWKrdHnvckBw\iCPQ1[tO{B1fW2xcjDj[YxtKHC{b3zp[oVz[XSrb36= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh2M{KxNUc,OTB6NEOyNVE9N2F-
Mia PaCa-2 cell MWTGeY5kfGmxbjDhd5NigQ>? M4r2XWlvcGmkaYTpc44hd2ZiTXnhJHBiS2FvMjDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9N|Yh|ryP NGfWcJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUC2N|YxQSd-MUGwOlM3ODl:L3G+
A2780 cell NUXX[VlDTnWwY4Tpc44h[XO|YYm= M{ft[WlvcGmkaYTpc44hd2ZiQUK3PFAh[2WubDDjcI9vd2enbnnjJIF{e2G778{MJGlEPTB;MUWg{txO M1n3UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzME[zOlA6Lz5zMUC2N|YxQTxxYU6=
HCT116 cell MUPGeY5kfGmxbjDhd5NigQ>? NIfPcFJKdmirYnn0bY9vKG:oIFjDWFEyPiClZXzsJINtd26xZ3XubYMh[XO|YYmsJGlEPTB;MUOg{txO Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTFyNkO2NFkoRjFzME[zOlA6RC:jPh?=
PC3 cell MlrxSpVv[3Srb36gZZN{[Xl? NH:yU2hKdmirYnn0bY9vKG:oIGDDN{Bk\WyuIHPsc45w\2WwaXOgZZN{[XluIFnDOVA:OTBizszN M13rcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzME[zOlA6Lz5zMUC2N|YxQTxxYU6=
K562 human leukemia cell M3\lN3Bzd2yrZnXyZZRqd25iYYPzZZk> MnzrTY5pcWKrdHnvckBw\iCNNU[yJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1yLkGzJO69VQ>? NVnxTJlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
MIP human colon carcinoma cell M1\BW2Z2dmO2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKE2LUDDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDsbY5mNCCLQ{WwQVAvOTJizszN M4jBUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A549 human lung carcinoma cell NF\Fd4pRem:uaX\ldoF1cW:wIHHzd4F6 MkLZTY5pcWKrdHnvckBw\iCDNUS5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF06PiCwTR?= NVSzO|VtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
CACO-2 human colon carcinoma cell NXL0boxUWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKEODQ1:tNkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTh4IH7N MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
M109 mouse lung carcinoma cell M1q4e3Bzd2yrZnXyZZRqd25iYYPzZZk> NYDWOINNUW6qaXLpeIlwdiCxZjDNNVA6KG2xdYPlJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16MDDuUS=> M2LZTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A2780/TAX-R human ovarian carcinoma cell MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 NYjmSHljUW6qaXLpeIlwdiCxZjDBNlc5OC:WQWitVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;N{igcm0> NFWwNow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
SKBR-3 human breast carcinoma cell MnnzVJJwdGmoZYLheIlwdiCjc4PhfS=> NXnXbVF6UW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? NITWO5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
A431 human squamous cell M3q2S3Bzd2yrZnXyZZRqd25iYYPzZZk> M2rqO2lvcGmkaYTpc44hd2ZiQUSzNUBpfW2jbjDzdZVidW:3czDj[YxtKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PzVibl2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
LX-1 human lung carcinoma NVr3Vm5QWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4\K[WlvcGmkaYTpc44hd2ZiTGitNUBpfW2jbjDseY5oKGOjcnPpco9u[SCycn;sbYZmemG2aX;uMEBKSzVyPUe1JI5O MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
MLF mouse lung fibroblast cell M4PyfXBzd2yrZnXyZZRqd25iYYPzZZk> MkPnTY5pcWKrdHnvckBw\iCPTF[gcY92e2VibIXu[{BncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04OiCwTR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
PC3 human prostate carcinoma cell M1S2bnBzd2yrZnXyZZRqd25iYYPzZZk> M3naTWlvcGmkaYTpc44hd2ZiUFOzJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;Nk[gcm0> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
MCF-7 human breast carcinoma cell MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NFfMUFdKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MmD3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
LS174T human colon carcinoma cell NEW0e2dRem:uaX\ldoF1cW:wIHHzd4F6 NWHudpJoUW6qaXLpeIlwdiCxZjDMV|E4PFRiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OUBvVQ>? NVPtZXRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
A2780/TAX-S human ovarian carcinoma cell MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MYLJcohq[mm2aX;uJI9nKEF{N{iwM3RCYC2VIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF03PSCwTR?= M{XhUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
A2780/DDP-S human ovarian carcinoma cell NYHoXo1vWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoXsTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTZibl2= M{nMT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|E{Lz5zMkG5NFMyOzxxYU6=
OVCAR-3 human ovarian carcinoma cell MWLQdo9tcW[ncnH0bY9vKGG|c3H5 MmfUTY5pcWKrdHnvckBw\iCRVlPBVk0{KGi3bXHuJI93[XKrYX6gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21OEBvVQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
CCRF-CEM human leukemia cell MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 NVTwdHoyUW6qaXLpeIlwdiCxZjDDR3JHNUOHTTDoeY1idiCuZYXr[Y1q[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTJibl2= NVex[5cyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
Hs 27 human fibroblast cell NHroUmxRem:uaX\ldoF1cW:wIHHzd4F6 NILOU5dKdmirYnn0bY9vKG:oIFjzJFI4KGi3bXHuJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVUyKG6P MnLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
HL60 human leukemia cell NYizWVllWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoTKTY5pcWKrdHnvckBw\iCKTE[wJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD12NjDuUS=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
ABAE human fibroblast cell NH7LTpNRem:uaX\ldoF1cW:wIHHzd4F6 NF7pTZlKdmirYnn0bY9vKG:oIFHCRWUhcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OFUhdk1? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
A2780/DDP-R human ovarian carcinoma cell M13EUXBzd2yrZnXyZZRqd25iYYPzZZk> MXrJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0{QCCwTR?= NWP4bVFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{OTNpPkGyNVkxOzF|PD;hQi=>
HCT116/VM46 human colon carcinoma cell NHfQOVBRem:uaX\ldoF1cW:wIHHzd4F6 Mor2TY5pcWKrdHnvckBw\iCKQ2SxNVYwXk12NjDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVIyKG6P Mm\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
HCT116 human colon carcinoma cell Mn;OVJJwdGmoZYLheIlwdiCjc4PhfS=> NUe5ZolbUW6qaXLpeIlwdiCxZjDIR3QyOTZiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2xPEBvVQ>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOxN{c,OTJzOUCzNVM9N2F-
HCT116/VP35 human colon carcinoma cell MXTQdo9tcW[ncnH0bY9vKGG|c3H5 Mki2TY5pcWKrdHnvckBw\iCKQ2SxNVYwXlB|NTDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVE4KG6P NGn4Oow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkG5NFMyOyd-MUKxPVA{OTN:L3G+
LNCaP human prostate carcinoma cell NVzPUlJzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnyyTY5pcWKrdHnvckBw\iCOTlPhVEBpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;u Mom4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNVMoRjF{MUmwN|E{RC:jPh?=
human A2780 cell line Mn3hVJJwdGmoZYLheIlwdiCjc4PhfS=> MoTGO|IhcA>? M2nMVGFvfGmycn;sbYZmemG2aY\lJIVn\mWldDDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGxibHnu[UB4[XNiZHX0[ZJucW6nZDDpckBiKHeqb3zlJINmdGxiN{KgbJIh[3m2b4TvfIlkcXS7IHHzd4F6NCCLQ{WwQVcyKG6P MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTB{N{i2N{c,OTVyMke4OlM9N2F-
human ovarian (A2780) cancer cell MV7DfZRwfG:6aXRCpIF{e2G7 NE\qe|dEgXSxdH;4bYMh\W[oZXP0JI9vKGi3bXHuJI93[XKrYX6gLGEzPzhyKTDjZY5k\XJiY3XscEBtcW6nLDDJR|UxRTdzIH7N NX;hb5RTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxNlU6PzFpPkG1NVI2QTdzPD;hQi=>
ID8 M4fFVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4S= M2r2XmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTWQ5KGOnbHzzMEBKSzVyPUCuNFA4|ryP M{X1dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUKzPFIyLz5zN{GyN|gzOTxxYU6=
MCF7 M4nYXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4S= MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOsJGlEPTB;MD6wNlbPxE1? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF{M{iyNUc,OTdzMkO4NlE9N2F-
Sf9 NWe2[YhVUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBkgWOuaX6gRU9ETEt{IHX4dJJme3OnZDDpci=> NWPRVmJGUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBkgWOuaX6gRU9ETEt{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE4xOTMQvF2= NF7YV|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{mwOFM3Pid-MUe5NFQ{PjZ:L3G+
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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 At the maximal tolerated dose of 10 mg/kg/day administered p.o. on days 1-4 and 7-11, Flavopiridol effects tumor regression in PRXF1337 and tumor stasis lasting for 4 weeks in PRXF1369. [4] After treatment with 7.5 mg/kg Flavopiridol bolus intravenous (IV) or intraperitoneal on each of 5 consecutive days, 11 out of 12 advanced stage subcutaneous (s.c.) human HL-60 xenografts undergo complete regressions, and animals remain disease-free several months after one course of Flavopiridol treatment. SUDHL-4 s.c. lymphomas treated with flavopiridol at 7.5 mg/kg bolus IV for 5 days undergo either major (two out of eight mice) or complete (four out of eight mice) regression, with two animals remaining disease-free for more than 60 days. The overall growth delay is 73.2%. Daily IV or IP administration of flavopiridol results in peak plasma levels of about 7 µM, followed by a progressive decline to approximately 100 nM in 8 hours.[6]

Protocol (from reference)

Kinase Assay:[1]
  • Recombinant CDKs Kinase Reactions:

    CDKs activities are determined in microtiter plates as follows. Forty μg Gst-Rb are mixed with different amounts of Flavopiridol and unlabeled ATP. Reactions are then started by the addition of an ammonium sulfate cut of the S100 fraction obtained from insect cells expressing recombinant human CDKs. The final reaction conditions are 10 mM MgCl2, 50 mM Tris-HCl (pH 7.5), and 1 mM DTT. The final concentration of ATP is adjusted accordingly. Radiolabeled ATP is used as a phosphoryl donor. The reaction is carried out for 2.5 minutes at 30 °C after addition of enzyme and then terminated with the addition of EDTA. The Gst-Rb is then captured with glutathione-Sepharose and the incorporated radioactivity is determined by liquid scintillation counting.

Cell Research:[2]
  • Cell lines: SUDHL4, SUDHL6, Jurkat, MOLT4, and HL60
  • Concentrations: 0, 100 500, 5000 nM
  • Incubation Time: 14 hours
  • Method: Cells grown at a density of 1 × 106 cells/mL are exposed to Flavopiridol for different concentrations and time periods. DNA is extracted. Briefly, cells are washed once with cold phosphate-buffered saline (PBS) and lysed with 3 mL lysis buffer (5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100) for 15 minutes at 4 °C. The chromatin of the cell lysates is isolated by centrifugation (20 minutes at 26,000g, 4 °C). The supernatants containing small DNA fragments are extracted sequentially with phenol, phenol:chloroform (1:1), and chloroform. Nucleic acids are precipitated in 0.5 M NaCl, 90% ethanol at -20 °C overnight. RNA is then digested by bovine RNAaseA (60 μg/mL). After sequential reextraction and reprecipitation, DNA is dissolved in 10 mM Tris-HCL (pH 7.5), 1 mM EDTA, 0.5% sodium dodecyl sulfate (SDS) before electrophoresis on 1.6% agarose gel.
Animal Research:[4] [6]
  • Animal Models: Human prostate cancer xenografts, PRXFI337 and PRXFI369, grown s.c. in nude mice [4] Human promyelocytic leukemia HL-60, human B-cell follicular lymphoma SUDHL-4, and acquired immunodeficiency syndrome (AIDS)-r
  • Dosages: 10 mg/kg/d [4]; 7.5 mg/kg/d [6]
  • Administration: p.o.[4]; i.p. or i.v. [6]

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 438.3
Formula

C21H20ClNO5.HCl

CAS No. 131740-09-5
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.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

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

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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