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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Cited by 16 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 NEfr[IlRem:uaX\ldoF1cW:wIHHzd4F6 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFnEPEBk\WyuczygTWM2OD15IH7N MkDqNVcyOjN6MkG=
Sf9 cells NYW5bFZVTnWwY4Tpc44h[XO|YYm= M{fPemlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgZ5lkdGmwIFGvR2RMOiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUGyJI5O M{O3TVE4QTB2M{[2
LNCaP human prostate carcinoma cell M1rJeHBzd2yrZnXyZZRqd25iYYPzZZk> NWLJWHFoUW6qaXLpeIlwdiCxZjDMUmNiWCCqdX3hckBxem:|dHH0[UBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9v NHvXcIYyOjF7MEOxNy=>
HCT116/VP35 human colon carcinoma cell MVTQdo9tcW[ncnH0bY9vKGG|c3H5 M4noVGlvcGmkaYTpc44hd2ZiSFPUNVE3N1[SM{WgbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0yPyCwTR?= NFnTZXoyOjF7MEOxNy=>
HCT116 human colon carcinoma cell NHT3d5lRem:uaX\ldoF1cW:wIHHzd4F6 M{[zNmlvcGmkaYTpc44hd2ZiSFPUNVE3KGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MUigcm0> M4C4c|EzOTlyM{Gz
HCT116/VM46 human colon carcinoma cell MWTQdo9tcW[ncnH0bY9vKGG|c3H5 M2D6XGlvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= NX;0bFBCOTJzOUCzNVM>
human A2780 cells M1vaWGN6fG:2b4jpZ:Kh[XO|YYm= M2X0[lI1KGh? NVzu[pJrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zOyCwTR?= NXzjOoU6OjN|MEG3Olc>
MCF7 cells NG\6NXJRem:uaX\ldoF1cW:wIHHzd4F6 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOsJGlEPTB;Mk[gcm0> MXKxO|EzOzh{MR?=
human MRC5 cells MoXHR5l1d3SxeHnjxsBie3OjeR?= NF7sWJE4OiCq NEHVR|lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlghdk1? NX2wO|BlOjN|MEG3Olc>
human A2780 cells M{TrOWN6fG:2b4jpZ:Kh[XO|YYm= MY[3NkBp Mo\pR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yPUBvVQ>? MXmyN|MxOTd4Nx?=
human A2780 cells MYrDfZRwfG:6aXRCpIF{e2G7 NYXKS4Q5PDhiaB?= NHX3TGJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVMyKG6P NHfrVFQzOzNyMUe2Oy=>
A2780/DDP-R human ovarian carcinoma cell NVPldW85WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0{QCCwTR?= M1LGR|EzOTlyM{Gz
human MRC5 cells M361OGN6fG:2b4jpZ:Kh[XO|YYm= Mne5OFghcA>? M2fDO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zPUBvVQ>? M4DWd|I{OzBzN{[3
ABAE human fibroblast cell NUjHOm1HWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3fkcGlvcGmkaYTpc44hd2ZiQVLBSUBpfW2jbjDmbYJzd2KuYYP0JINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OUBvVQ>? NWT6ZYZuOTJzOUCzNVM>
HL60 human leukemia cell MYjQdo9tcW[ncnH0bY9vKGG|c3H5 M33TXmlvcGmkaYTpc44hd2ZiSFy2NEBpfW2jbjDs[ZVs\W2rYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NE[gcm0> M1LR[FEzOTlyM{Gz
human MRC5 cells NX31Z2pzS3m2b4TvfIlkyqCjc4PhfS=> NGW2W4YzPCCq M1;xb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME20PUBvVQ>? MnvwNlM{ODF5Nke=
Hs 27 human fibroblast cell NXfue|hvWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKEi|IEK3JIh2dWGwIH\pZpJw[myjc4SgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUWxJI5O M3zKW|EzOTlyM{Gz
CCRF-CEM human leukemia cell MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M4fxNWlvcGmkaYTpc44hd2ZiQ1PSSk1ETU1iaIXtZY4hdGW3a3XtbYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVUzKG6P MlXsNVIyQTB|MUO=
OVCAR-3 human ovarian carcinoma cell NY\pOmxrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXzUd5FiUW6qaXLpeIlwdiCxZjDPWmNCWi1|IHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02PCCwTR?= NUK2b3ROOTJzOUCzNVM>
A2780/DDP-S human ovarian carcinoma cell Mke3VJJwdGmoZYLheIlwdiCjc4PhfS=> NGDhU5hKdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3TJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD13NjDuUS=> Mm\XNVIyQTB|MUO=
human HMEC1 cells NVvsSnd2S3m2b4TvfIlkyqCjc4PhfS=> MV[yOEBp MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[xJI5O NImxdYszOzNyMUe2Oy=>
human HMEC1 cells MlO4R5l1d3SxeHnjxsBie3OjeR?= NH\3O4s1QCCq NEXnWlREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYzKG6P NGWxTVgzOzNyMUe2Oy=>
A2780/TAX-S human ovarian carcinoma cell MmTQVJJwdGmoZYLheIlwdiCjc4PhfS=> M2nmSGlvcGmkaYTpc44hd2ZiQUK3PFAwXEG[LWOgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ3IH7N Mmm0NVIyQTB|MUO=
LS174T human colon carcinoma cell MkPBVJJwdGmoZYLheIlwdiCjc4PhfS=> M17acGlvcGmkaYTpc44hd2ZiTGOxO|RVKGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NkWgcm0> NVe4bHYyOTJzOUCzNVM>
MCF-7 human breast carcinoma cell NEC3eWVRem:uaX\ldoF1cW:wIHHzd4F6 NIDXWnZKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O NES1fJEyOjF7MEOxNy=>
human HMEC1 cells M13BZ2N6fG:2b4jpZ:Kh[XO|YYm= M2\qXlczKGh? NXLaOFM4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE2HQ{GgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF03PiCwTR?= NVTncnJrOjN|MEG3Olc>
PC3 human prostate carcinoma cell MljjVJJwdGmoZYLheIlwdiCjc4PhfS=> MVHJcohq[mm2aX;uJI9nKFCFMzDoeY1idiCycn;zeIF1\SClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N M{D3XFEzOTlyM{Gz
human A2780 cell line MmS0VJJwdGmoZYLheIlwdiCjc4PhfS=> MkTrO|IhcA>? NHXSNWxCdnSrcILvcIln\XKjdHn2[UBm\m[nY4SgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgbY4h[SC5aH;s[UBk\WyuIEeyJIhzKGO7dH;0c5hq[2m2eTDhd5NigSxiSVO1NF04OSCwTR?= NYDPe5FuOTVyMke4OlM>
human ovarian (A2780) cancer cell NF[xR|BEgXSxdH;4bYPDqGG|c3H5 MmDBR5l1d3SxeHnjJIVn\mWldDDvckBpfW2jbjDveoFzcWGwIDjBNlc5OCliY3HuZ4VzKGOnbHygcIlv\SxiSVO1NF04OSCwTR?= M1P2dVE2OTJ3OUex
MLF mouse lung fibroblast cell NHu2W4dRem:uaX\ldoF1cW:wIHHzd4F6 MkW1TY5pcWKrdHnvckBw\iCPTF[gcY92e2VibIXu[{BncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04OiCwTR?= NETP[GQyOjF7MEOxNy=>
human NCI60 cells MYTQdo9tcW[ncnH0bY9vKGG|c3H5 M1TVO|czKGh? NVHQTHVVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF04PC55IH7N NV\4S4J3OjFyOEC3NFM>
LX-1 human lung carcinoma M4qzbHBzd2yrZnXyZZRqd25iYYPzZZk> NIXOfm1KdmirYnn0bY9vKG:oIFzYMVEhcHWvYX6gcJVv\yClYYLjbY5wdWFicILvcIln\XKjdHnvckwhUUN3ME23OUBvVQ>? NVP4VnB6OTJzOUCzNVM>
A431 human squamous cell NW\NSlE5WHKxbHnm[ZJifGmxbjDhd5NigQ>? MnyzTY5pcWKrdHnvckBw\iCDNEOxJIh2dWGwIIPxeYFud3W|IHPlcIwh[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04PSCwTR?= M1TU[lEzOTlyM{Gz
SKBR-3 human breast carcinoma cell NV;zeJd6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NWnodnlGUW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? M2LncVEzOTlyM{Gz
A2780/TAX-R human ovarian carcinoma cell M3HHZXBzd2yrZnXyZZRqd25iYYPzZZk> Mm\5TY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Pzhibl2= MUixNlE6ODNzMx?=
M109 mouse lung carcinoma cell M{XvOHBzd2yrZnXyZZRqd25iYYPzZZk> NIq1V2ZKdmirYnn0bY9vKG:oIF2xNFkhdW:3c3WgcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRThyIH7N MoXKNVIyQTB|MUO=
CACO-2 human colon carcinoma cell MnToVJJwdGmoZYLheIlwdiCjc4PhfS=> MlnGTY5pcWKrdHnvckBw\iCFQVPPMVIhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16NjDuUS=> NV\HdZB[OTJzOUCzNVM>
A549 human lung carcinoma cell NYfhO2J3WHKxbHnm[ZJifGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKEF3NEmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVk3KG6P Mn\GNVIyQTB|MUO=
MIP human colon carcinoma cell MUHGeY5kfGmxbjDhd5NigQ>? NXjUfoxoUW6qaXLpeIlwdiCxZjDNTXAhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwhdGmwZTygTWM2OD1yLkGyJO69VQ>? Mon4NVIyQTB|MUO=
K562 human leukemia cell MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NXPHTFBEUW6qaXLpeIlwdiCxZjDLOVYzKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlE{KM7:TR?= MmnyNVIyQTB|MUO=
MCF-7 tumor cell M1PEOXBzd2yrZnXyZZRqd25iYYPzZZk> MWHJcohq[mm2aX;uJI9nKE2FRj23JJR2dW:{IHPlcIwheHKxbHnm[ZJifGmxbh?= MnHuNVA5PDN{MUG=
human NCI60 cells MlXPVJJwdGmoZYLheIlwdiCjc4PhfS=> MUi3NkBp MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FSU[wJINmdGy|IHHzd4V{e2WmIHHzJIxmfGijbDDl[oZm[3RiYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGxEPTB;MD65NFQh|ryP MnTUNlExQDB5MEO=
PC3 cell MonUSpVv[3Srb36gZZN{[Xl? Mon6TY5pcWKrdHnvckBw\iCSQ{OgZ4VtdCClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVExKM7:TR?= Mnq4NVExPjN4MEm=
HCT116 cell M3;tbGZ2dmO2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKEiFVEGxOkBk\WyuIHPsc45w\2WwaXOgZZN{[XluIFnDOVA:OTNizszN Ml61NVExPjN4MEm=
A2780 cell MVLGeY5kfGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKEF{N{iwJINmdGxiY3zvco9o\W6rYzDhd5Nige,:jDDJR|UxRTF3IN88US=> MXGxNVA3OzZyOR?=
Mia PaCa-2 cell MXHGeY5kfGmxbjDhd5NigQ>? M2L2VWlvcGmkaYTpc44hd2ZiTXnhJHBiS2FvMjDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9N|Yh|ryP NUHhdYVzOTFyNkO2NFk>
human A2780 cells NG\ke4hHfW6ldHnvckBie3OjeR?= M2n1dGlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJG5RVSCyaH;zdIhwenmuYYTpc44h[XRidHjyNVk6KGmwIHj1cYFvKEF{N{iwJINmdGy| NUHMPHdPOTh2Nkm4NFk>
human A2780 cells NWrV[4Q4TnWwY4Tpc44h[XO|YYm= MkjoNlQhcA>? NWfjTG93UW6qaXLpeIlwdiCxZjDj[IsudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IITodlgzOSCrbjDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB{NDDodpM> MWexPFQ3QThyOR?=

... 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