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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  • (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.

    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.

  • 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.

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 MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NWfW[pV1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBKTDhiY3XscJMtKEmFNUC9O{BvVQ>? M3vZ[FE4OTJ|OEKx
Sf9 cells MmXpSpVv[3Srb36gZZN{[Xl? M1vFeGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgZ5lkdGmwIFGvR2RMOiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUGyJI5O NHuyW|YyPzlyNEO2Oi=>
LNCaP human prostate carcinoma cell MkPkVJJwdGmoZYLheIlwdiCjc4PhfS=> NFO2RYxKdmirYnn0bY9vKG:oIFzOR4FRKGi3bXHuJJBzd3O2YYTlJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44> NIGxVIQyOjF7MEOxNy=>
HCT116/VP35 human colon carcinoma cell MYPQdo9tcW[ncnH0bY9vKGG|c3H5 NYj0SY9VUW6qaXLpeIlwdiCxZjDIR3QyOTZxVmCzOUBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTF5IH7N NWPhVpZzOTJzOUCzNVM>
HCT116 human colon carcinoma cell NETYXJhRem:uaX\ldoF1cW:wIHHzd4F6 Mn7YTY5pcWKrdHnvckBw\iCKQ2SxNVYhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1zODDuUS=> NGPBU5QyOjF7MEOxNy=>
HCT116/VM46 human colon carcinoma cell NEjaOGJRem:uaX\ldoF1cW:wIHHzd4F6 NW[yWJhvUW6qaXLpeIlwdiCxZjDIR3QyOTZxVl20OkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTJzIH7N M1zGPFEzOTlyM{Gz
human A2780 cells NI\nSVBEgXSxdH;4bYPDqGG|c3H5 NEjQe3IzPCCq NWrI[WxKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zOyCwTR?= MUGyN|MxOTd4Nx?=
MCF7 cells M3e2bnBzd2yrZnXyZZRqd25iYYPzZZk> NUnqN2g2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOS0Z5IHPlcIx{NCCLQ{WwQVI3KG6P MV6xO|EzOzh{MR?=
human MRC5 cells MlHXR5l1d3SxeHnjxsBie3OjeR?= MY[3NkBp NFjWXZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlghdk1? MoHvNlM{ODF5Nke=
human A2780 cells MnzVR5l1d3SxeHnjxsBie3OjeR?= NH;yVJE4OiCq NVPseHJoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zQSCwTR?= NGD0Z3MzOzNyMUe2Oy=>
human A2780 cells NETn[FlEgXSxdH;4bYPDqGG|c3H5 NWnB[WZEPDhiaB?= MorGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zNUBvVQ>? NGeySIMzOzNyMUe2Oy=>
A2780/DDP-R human ovarian carcinoma cell MmDTVJJwdGmoZYLheIlwdiCjc4PhfS=> MVnJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0{QCCwTR?= NUfZVVE3OTJzOUCzNVM>
human MRC5 cells M{XaXGN6fG:2b4jpZ:Kh[XO|YYm= NHe5[Wc1QCCq MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> NYfHPGNnOjN|MEG3Olc>
ABAE human fibroblast cell M4LD[3Bzd2yrZnXyZZRqd25iYYPzZZk> MYPJcohq[mm2aX;uJI9nKEGEQVWgbJVu[W5iZnnido9jdGG|dDDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NEWgcm0> Mnj1NVIyQTB|MUO=
HL60 human leukemia cell MWrQdo9tcW[ncnH0bY9vKGG|c3H5 NVzN[|R4UW6qaXLpeIlwdiCxZjDIUFYxKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OkBvVQ>? M2Hy[|EzOTlyM{Gz
human MRC5 cells M1[xdmN6fG:2b4jpZ:Kh[XO|YYm= NEHOblAzPCCq Ml\ZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUS5JI5O MlPONlM{ODF5Nke=
Hs 27 human fibroblast cell MojtVJJwdGmoZYLheIlwdiCjc4PhfS=> M3j3Z2lvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? NFrO[ZUyOjF7MEOxNy=>
CCRF-CEM human leukemia cell NVLUXlB6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3rISGlvcGmkaYTpc44hd2ZiQ1PSSk1ETU1iaIXtZY4hdGW3a3XtbYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVUzKG6P NG\l[lcyOjF7MEOxNy=>
OVCAR-3 human ovarian carcinoma cell NGe0SGdRem:uaX\ldoF1cW:wIHHzd4F6 MmDQTY5pcWKrdHnvckBw\iCRVlPBVk0{KGi3bXHuJI93[XKrYX6gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21OEBvVQ>? NFzkW3EyOjF7MEOxNy=>
A2780/DDP-S human ovarian carcinoma cell Mof0VJJwdGmoZYLheIlwdiCjc4PhfS=> NFr0e3pKdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3TJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD13NjDuUS=> NHW2PWgyOjF7MEOxNy=>
human HMEC1 cells MYLDfZRwfG:6aXRCpIF{e2G7 NFiwT|MzPCCq NGTpcnVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYyKG6P M3fld|I{OzBzN{[3
human HMEC1 cells NVy5Voh7S3m2b4TvfIlkyqCjc4PhfS=> NHHZeI81QCCq NXTkVGtCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE2HQ{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF03OiCwTR?= NF;2XmMzOzNyMUe2Oy=>
A2780/TAX-S human ovarian carcinoma cell M{njXnBzd2yrZnXyZZRqd25iYYPzZZk> Mn:1TY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PjVibl2= MVGxNlE6ODNzMx?=
LS174T human colon carcinoma cell MlTGVJJwdGmoZYLheIlwdiCjc4PhfS=> MmXiTY5pcWKrdHnvckBw\iCOU{G3OHQhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NTDuUS=> NXvTSFhJOTJzOUCzNVM>
MCF-7 human breast carcinoma cell NEXUR4lRem:uaX\ldoF1cW:wIHHzd4F6 NXHYSm4{UW6qaXLpeIlwdiCxZjDNR2YuPyCqdX3hckBjemWjc4SgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OkBvVQ>? MX[xNlE6ODNzMx?=
human HMEC1 cells NXniSYdqS3m2b4TvfIlkyqCjc4PhfS=> Moe2O|IhcA>? MoiyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTG1GSzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME22OkBvVQ>? NECzRokzOzNyMUe2Oy=>
PC3 human prostate carcinoma cell NFWzV3RRem:uaX\ldoF1cW:wIHHzd4F6 NUDJXZVKUW6qaXLpeIlwdiCxZjDQR|MhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OkBvVQ>? NYnmRYNuOTJzOUCzNVM>
human A2780 cell line NEm2bHFRem:uaX\ldoF1cW:wIHHzd4F6 NUGzSI15PzJiaB?= Mn\tRY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9O|Ehdk1? NF60ZYoyPTB{N{i2Ny=>
human ovarian (A2780) cancer cell NWnmPFQ3S3m2b4TvfIlkyqCjc4PhfS=> MVHDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P NYP0NGl5OTVzMkW5O|E>
MLF mouse lung fibroblast cell NGHQSm1Rem:uaX\ldoF1cW:wIHHzd4F6 MVvJcohq[mm2aX;uJI9nKE2ORjDtc5V{\SCudX7nJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVczKG6P MWOxNlE6ODNzMx?=
human NCI60 cells NIq1PIpRem:uaX\ldoF1cW:wIHHzd4F6 MX:3NkBp NYD5SZg4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF04PC55IH7N M32we|IyODhyN{Cz
LX-1 human lung carcinoma M3u4U3Bzd2yrZnXyZZRqd25iYYPzZZk> MWrJcohq[mm2aX;uJI9nKEy[LUGgbJVu[W5ibIXu[{Bk[XKlaX7vcYEheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> M3\y[VEzOTlyM{Gz
A431 human squamous cell MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 MVLJcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P MliwNVIyQTB|MUO=
SKBR-3 human breast carcinoma cell M4DYNnBzd2yrZnXyZZRqd25iYYPzZZk> NHzXV3dKdmirYnn0bY9vKG:oIGPLRnIuOyCqdX3hckBjemWjc4SgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME23O{BvVQ>? MU[xNlE6ODNzMx?=
A2780/TAX-R human ovarian carcinoma cell NF7wc3RRem:uaX\ldoF1cW:wIHHzd4F6 MnrETY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Pzhibl2= MVixNlE6ODNzMx?=
M109 mouse lung carcinoma cell M1;pWXBzd2yrZnXyZZRqd25iYYPzZZk> NIHkfIpKdmirYnn0bY9vKG:oIF2xNFkhdW:3c3WgcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRThyIH7N MoXtNVIyQTB|MUO=
CACO-2 human colon carcinoma cell M{H1bXBzd2yrZnXyZZRqd25iYYPzZZk> MXLJcohq[mm2aX;uJI9nKEODQ1:tNkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTh4IH7N NETXV3cyOjF7MEOxNy=>
A549 human lung carcinoma cell MUDQdo9tcW[ncnH0bY9vKGG|c3H5 M1nRV2lvcGmkaYTpc44hd2ZiQUW0PUBpfW2jbjDseY5oKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:QTZibl2= NEnQOXYyOjF7MEOxNy=>
MIP human colon carcinoma cell NV7vOHh1TnWwY4Tpc44h[XO|YYm= NHPkZWhKdmirYnn0bY9vKG:oIF3JVEBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBtcW6nLDDJR|UxRTBwMUKg{txO M2m5PVEzOTlyM{Gz
K562 human leukemia cell MkDBVJJwdGmoZYLheIlwdiCjc4PhfS=> M4\Bd2lvcGmkaYTpc44hd2ZiS{W2NkBpfW2jbjDs[ZVs\W2rYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD6xN{DPxE1? M{H0UVEzOTlyM{Gz
MCF-7 tumor cell MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NYOxbY5DUW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> MYCxNFg1OzJzMR?=
human NCI60 cells NYjWTGJjWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYW3NkBp NVKwSmNJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bie3Onc4Pl[EBieyCuZYToZYwh\W[oZXP0JIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCOQ{WwQVAvQTB2IN88US=> NUDSPVE1OjFyOEC3NFM>
PC3 cell M3T3WGZ2dmO2aX;uJIF{e2G7 M4C0UWlvcGmkaYTpc44hd2ZiUFOzJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0yOCEQvF2= MX2xNVA3OzZyOR?=
HCT116 cell MX;GeY5kfGmxbjDhd5NigQ>? NYTzbodzUW6qaXLpeIlwdiCxZjDIR3QyOTZiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUGzJO69VQ>? M2GyeVEyODZ|NkC5
A2780 cell M{nK[WZ2dmO2aX;uJIF{e2G7 NIjLT5hKdmirYnn0bY9vKG:oIFGyO|gxKGOnbHygZ4xwdm:pZX7pZ{Bie3Ojef-8kEBKSzVyPUG1JO69VQ>? Mnm3NVExPjN4MEm=
Mia PaCa-2 cell MVjGeY5kfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKE2rYTDQZWNiNTJiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUO2JO69VQ>? NIfTZngyOTB4M{[wPS=>
human A2780 cells NUHkOGlQTnWwY4Tpc44h[XO|YYm= M{j6VmlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJG5RVSCyaH;zdIhwenmuYYTpc44h[XRidHjyNVk6KGmwIHj1cYFvKEF{N{iwJINmdGy| M3\KNFE5PDZ7OEC5
human A2780 cells MVzGeY5kfGmxbjDhd5NigQ>? MoX0NlQhcA>? MWLJcohq[mm2aX;uJI9nKGOmaz3t[YRq[XSnZDDSZkBxcG:|cHjvdplt[XSrb36gZZQhfGi{OEKxJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFI1KGi{cx?= NHLHSIYyQDR4OUiwPS=>

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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:
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
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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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 )

  • C1
    V1
    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00094978 Terminated Carcinoma, Small Cell|Carcinoma, Non-Small-Cell Lung|Esophageal Neoplasms|Mesothelioma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 25, 2004 Phase 1
NCT00445341 Completed Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 2007 Phase 1|Phase 2
NCT00083122 Completed Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Primary Peritoneal Cavity Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Primary Peritoneal Cavity Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Primary Peritoneal Cavity Cancer|Stage IV Ovarian Epithelial Cancer|Stage IV Primary Peritoneal Cavity Cancer National Cancer Institute (NCI) April 2004 Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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