Flavopiridol HCl

Catalog No.S2679 Synonyms: NSC 649890 HCl

Flavopiridol HCl Chemical Structure

Molecular Weight(MW): 438.3

Flavopiridol HCl 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. Phase 1/2.

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In DMSO USD 100 In stock
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Cited by 18 Publications

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  • Comparative efficacy of anticancer therapies (Flavopiridol, vincristine, daunorubicin, et al.) in NMC vs non-NMC cell lines. Mean IC50 (± s.e.m.) of the indicated agents in three NMC (PER-403, PER-624, and PER-704) and two non-NMC cell lines (PER-535 and SAOS2), ***P<0.001, unpaired t-test, corrected for multiple testing.

    Br J Cancer 2014 110(5), 1189-98. Flavopiridol HCl purchased from Selleck.

  • RPMI-8226 cells were treated with the indicated CDK inhibitors for 8 hours. Western blots are shown. The following drug concentrations were used: SLM6 at 250 nM, flavopiridol at 250 nM, roscovitine at 5 uM, purvalanol A at 10 uM, and alsterpaullone at 5 uM.

    Mol Cancer Ther 2012 11(11), 2321-2330. Flavopiridol HCl purchased from Selleck.

  • (C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50μM) or 0.2% DMSO as control from 18 to 40 hpf. One hundred to one hundred fifty embryos were treated with each compound. Representative images of live embryos are shown with gross morphology (Right) and pituitary Pomc-GFP–positive cells at higher magnification (Left) at 40 hpf. Embryos exposed to flavopiridol developed early developmental defect before pituitary POMC cell ontogeny occurs. (D) Relative expression of pituitary Pomc-eGFP fluorescence analyzed using Volocity 5.2 software (Improvision; mean ± SE of relative expression, n = 7). (E) R-roscovitine specifically suppresses expansion of pituitary POMC cells overexpressing zPttg from 18 to 48 hpf. Double transgenic Tg:Pomc-Pttg;Prl-RFP embryos were generated by breeding Tg:Pomc-Pttg fish with a previously generated PRL-RFP transgenic line, in which RFP was targeted to pituitary lactotrophs by a zebrafish Prolactin promoter (34). Representative fluorescent microscopy of pituitary POMC-eGFP (a and b) and PRL-RFP (c and d) expression in live Tg:Pomc-Pttg; Pomc-eGFP and Tg:Pomc-Pttg;Prl-RFP embryos treated with 0.2% DMSO (a and c) or 50 μM R-roscovitine (b and d). (F) Relative expression of pituitary POMC-eGFP or PRL-RFP fluorescence were analyzed (mean ± SE of relative expression; n = 10). Results represent one of three similar experiments;*P < 0.02 and **P < 0.000005. (Scale bar, 50 μm.)

     

     

    PNAS 2011 108, 8417. Flavopiridol HCl purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description Flavopiridol HCl 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. 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
ID8 cells NXW4PYllWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFnEPEBk\WyuczygTWM2OD15IH7N M3fVZ|E4OTJ|OEKx
Sf9 cells M3PkbWZ2dmO2aX;uJIF{e2G7 NInKTWFKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIN6[2yrbjDBM2NFUzJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2xNkBvVQ>? NUHPeWh3OTd7MESzOlY>
LNCaP human prostate carcinoma cell M{fCR3Bzd2yrZnXyZZRqd25iYYPzZZk> M3PsfmlvcGmkaYTpc44hd2ZiTF7DZXAhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvci=> M2DO[|EzOTlyM{Gz
HCT116/VP35 human colon carcinoma cell NUDQZVZNWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKEiFVEGxOk9XWDN3IHj1cYFvKGOxbH;uJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9NVchdk1? NXjrbotwOTJzOUCzNVM>
HCT116 human colon carcinoma cell NFq2boVRem:uaX\ldoF1cW:wIHHzd4F6 M{\xVWlvcGmkaYTpc44hd2ZiSFPUNVE3KGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MUigcm0> NXrzZ2hVOTJzOUCzNVM>
HCT116/VM46 human colon carcinoma cell NVThV29DWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1Ho[2lvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= NH:xfnoyOjF7MEOxNy=>
human A2780 cells MonqR5l1d3SxeHnjxsBie3OjeR?= Mon5NlQhcA>? NXO1SoFzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zOyCwTR?= NGnDVGszOzNyMUe2Oy=>
MCF7 cells M2\tUnBzd2yrZnXyZZRqd25iYYPzZZk> MknPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNR2Y4KGOnbHzzMEBKSzVyPUK2JI5O NV3IR3VDOTdzMkO4NlE>
human MRC5 cells NE\5NJFEgXSxdH;4bYPDqGG|c3H5 MV:3NkBp NGDtPWxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlghdk1? NGG2T2MzOzNyMUe2Oy=>
human A2780 cells MUDDfZRwfG:6aXRCpIF{e2G7 MoXqO|IhcA>? MkTxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yPUBvVQ>? MXqyN|MxOTd4Nx?=
human A2780 cells MWPDfZRwfG:6aXRCpIF{e2G7 Mk\SOFghcA>? NV7KT2djS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0{OSCwTR?= MVeyN|MxOTd4Nx?=
A2780/DDP-R human ovarian carcinoma cell MVPQdo9tcW[ncnH0bY9vKGG|c3H5 Mli1TY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Ozhibl2= NFfrWZAyOjF7MEOxNy=>
human MRC5 cells NVn0PVk2S3m2b4TvfIlkyqCjc4PhfS=> MoDzOFghcA>? MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> M3vJRVI{OzBzN{[3
ABAE human fibroblast cell Mlv4VJJwdGmoZYLheIlwdiCjc4PhfS=> MnjQTY5pcWKrdHnvckBw\iCDQlHFJIh2dWGwIH\pZpJw[myjc4SgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUS1JI5O MkLKNVIyQTB|MUO=
HL60 human leukemia cell MnLxVJJwdGmoZYLheIlwdiCjc4PhfS=> NWT5fYVmUW6qaXLpeIlwdiCxZjDIUFYxKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OkBvVQ>? MUSxNlE6ODNzMx?=
human MRC5 cells NVXqdWNXS3m2b4TvfIlkyqCjc4PhfS=> Mlq2NlQhcA>? MlziR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUS5JI5O NFTSRXMzOzNyMUe2Oy=>
Hs 27 human fibroblast cell MXnQdo9tcW[ncnH0bY9vKGG|c3H5 M4f3S2lvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? NV3mS3JxOTJzOUCzNVM>
CCRF-CEM human leukemia cell NIHvNVBRem:uaX\ldoF1cW:wIHHzd4F6 NEPVeYJKdmirYnn0bY9vKG:oIFPDVmYuS0WPIHj1cYFvKGyndXvlcYliKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OiCwTR?= MXmxNlE6ODNzMx?=
OVCAR-3 human ovarian carcinoma cell M3TiTnBzd2yrZnXyZZRqd25iYYPzZZk> NGDsNY9KdmirYnn0bY9vKG:oIF;WR2FTNTNiaIXtZY4hd3[jcnnhckBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVU1KG6P M3f2TFEzOTlyM{Gz
A2780/DDP-S human ovarian carcinoma cell MWTQdo9tcW[ncnH0bY9vKGG|c3H5 MYjJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2VIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02PiCwTR?= NWnMcoRZOTJzOUCzNVM>
human HMEC1 cells NHjoWIZEgXSxdH;4bYPDqGG|c3H5 M4L2[VI1KGh? NHLrNGxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYyKG6P NITrOZAzOzNyMUe2Oy=>
human HMEC1 cells NEGyXoxEgXSxdH;4bYPDqGG|c3H5 NWPENWRDPDhiaB?= MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[yJI5O NF;lN28zOzNyMUe2Oy=>
A2780/TAX-S human ovarian carcinoma cell NX7pbXpsWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2DrWmlvcGmkaYTpc44hd2ZiQUK3PFAwXEG[LWOgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ3IH7N M4T0UVEzOTlyM{Gz
LS174T human colon carcinoma cell MnH1VJJwdGmoZYLheIlwdiCjc4PhfS=> Ml74TY5pcWKrdHnvckBw\iCOU{G3OHQhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NTDuUS=> NWDZdVJTOTJzOUCzNVM>
MCF-7 human breast carcinoma cell M{TwOXBzd2yrZnXyZZRqd25iYYPzZZk> MYrJcohq[mm2aX;uJI9nKE2FRj23JIh2dWGwIHLy[YF{fCClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N NFP3UIoyOjF7MEOxNy=>
human HMEC1 cells NEjuTHJEgXSxdH;4bYPDqGG|c3H5 NX6zfpd{PzJiaB?= NFvuNotEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVY3KG6P NXHHSVM1OjN|MEG3Olc>
PC3 human prostate carcinoma cell NUfBd|RVWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml2yTY5pcWKrdHnvckBw\iCSQ{OgbJVu[W5icILvd5RifGViY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NjDuUS=> NH3YS4cyOjF7MEOxNy=>
human A2780 cell line MYTQdo9tcW[ncnH0bY9vKGG|c3H5 MmfEO|IhcA>? NWryWYtmSW62aYDyc4xq\mW{YYTpeoUh\W[oZXP0JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubDDsbY5mKHejczDk[ZRmem2rbnXkJIlvKGFid3jvcIUh[2WubDC3NkBpeiCleYTveI95cWOrdImgZZN{[XluIFnDOVA:PzFibl2= MnnVNVUxOjd6NkO=
human ovarian (A2780) cancer cell NGPUXWJEgXSxdH;4bYPDqGG|c3H5 MYDDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P NYLJVGNFOTVzMkW5O|E>
MLF mouse lung fibroblast cell MWfQdo9tcW[ncnH0bY9vKGG|c3H5 M{jITWlvcGmkaYTpc44hd2ZiTVzGJI1wfXOnIHz1coch\mmkcn;icIF{fCClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PzJibl2= M2T4RVEzOTlyM{Gz
human NCI60 cells NH3ObJJRem:uaX\ldoF1cW:wIHHzd4F6 MX:3NkBp M2jDb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9O|QvPyCwTR?= NYHoZpI4OjFyOEC3NFM>
LX-1 human lung carcinoma MmTZVJJwdGmoZYLheIlwdiCjc4PhfS=> Mnv3TY5pcWKrdHnvckBw\iCOWD2xJIh2dWGwIHz1coch[2G{Y3nuc41iKHC{b3zp[oVz[XSrb36sJGlEPTB;N{Wgcm0> M2\jR|EzOTlyM{Gz
A431 human squamous cell M3:2WHBzd2yrZnXyZZRqd25iYYPzZZk> NHfGVIVKdmirYnn0bY9vKG:oIFG0N|EhcHWvYX6gd5F2[W2xdYOgZ4VtdCClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTd3IH7N MnrKNVIyQTB|MUO=
SKBR-3 human breast carcinoma cell Mke0VJJwdGmoZYLheIlwdiCjc4PhfS=> NWPycGMxUW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? NGXtXYgyOjF7MEOxNy=>
A2780/TAX-R human ovarian carcinoma cell Mnz3VJJwdGmoZYLheIlwdiCjc4PhfS=> MnHBTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Pzhibl2= M2Dq[VEzOTlyM{Gz
M109 mouse lung carcinoma cell NWnPSWg5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NYjZPHJiUW6qaXLpeIlwdiCxZjDNNVA6KG2xdYPlJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16MDDuUS=> MonnNVIyQTB|MUO=
CACO-2 human colon carcinoma cell NUfTS4dVWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXrGblVxUW6qaXLpeIlwdiCxZjDDRWNQNTJiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME24OkBvVQ>? M2fmWFEzOTlyM{Gz
A549 human lung carcinoma cell NIrwfY1Rem:uaX\ldoF1cW:wIHHzd4F6 NEP3VVhKdmirYnn0bY9vKG:oIFG1OFkhcHWvYX6gcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTl4IH7N NF\Xb48yOjF7MEOxNy=>
MIP human colon carcinoma cell M3HlfmZ2dmO2aX;uJIF{e2G7 Mn:0TY5pcWKrdHnvckBw\iCPSWCgbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygcIlv\SxiSVO1NF0xNjF{IN88US=> M4X0UlEzOTlyM{Gz
K562 human leukemia cell MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 M3i3TWlvcGmkaYTpc44hd2ZiS{W2NkBpfW2jbjDs[ZVs\W2rYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD6xN{DPxE1? NG\RdlgyOjF7MEOxNy=>
MCF-7 tumor cell MlHaVJJwdGmoZYLheIlwdiCjc4PhfS=> NXPPd5FyUW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> NUjP[IdvOTB6NEOyNVE>
human NCI60 cells NHzhNohRem:uaX\ldoF1cW:wIHHzd4F6 MkfiO|IhcA>? M{PnRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZZN{\XO|ZXSgZZMhdGW2aHHsJIVn\mWldDDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhVEN3ME2wMlkxPCEQvF2= M1PxNlIyODhyN{Cz
PC3 cell MV\GeY5kfGmxbjDhd5NigQ>? MofSTY5pcWKrdHnvckBw\iCSQ{OgZ4VtdCClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVExKM7:TR?= MV6xNVA3OzZyOR?=
HCT116 cell NECxeXlHfW6ldHnvckBie3OjeR?= Moe0TY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> MWqxNVA3OzZyOR?=
A2780 cell NEjXcm9HfW6ldHnvckBie3OjeR?= MorrTY5pcWKrdHnvckBw\iCDMke4NEBk\WyuIHPsc45w\2WwaXOgZZN{[XoxvJygTWM2OD1zNTFOwG0> MoS1NVExPjN4MEm=
Mia PaCa-2 cell MWjGeY5kfGmxbjDhd5NigQ>? NFrINYFKdmirYnn0bY9vKG:oIF3pZUBR[UOjLUKgZ4VtdCClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVM3KM7:TR?= MV2xNVA3OzZyOR?=
human A2780 cells MYTGeY5kfGmxbjDhd5NigQ>? MlnoTY5pcWKrdHnvckBw\iClZHutcYVlcWG2ZXSgUnBOKHCqb4PwbI9zgWyjdHnvckBifCC2aIKxPVkhcW5iaIXtZY4hSTJ5OECgZ4VtdHN? M1rCZVE5PDZ7OEC5
human A2780 cells M2OyNWZ2dmO2aX;uJIF{e2G7 NUf0PWdYOjRiaB?= MoLHTY5pcWKrdHnvckBw\iClZHutcYVlcWG2ZXSgVoIheGixc4Doc5J6dGG2aX;uJIF1KHSqckiyNUBqdiCqdX3hckBCOjd6MDDj[YxteyCjZoTldkAzPCCqcoO= M2jId|E5PDZ7OEC5

... 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
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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[4] [6]
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  • 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
  • Formulation: Water [4]; 1% DMSO [6]
  • Dosages: 10 mg/kg/d [4]; 7.5 mg/kg/d [6]
  • Administration: p.o.[4]; i.p. or i.v. [6]
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (200.77 mM)
Water Insoluble
Ethanol Insoluble
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

* 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 438.3
Formula

C21H20ClNO5.HCl

CAS No. 131740-09-5
Storage powder
in solvent
Synonyms NSC 649890 HCl

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID