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 11 Publications

3 Customer Reviews

  • 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 M3nSbnBzd2yrZnXyZZRqd25iYYPzZZk> MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFnEPEBk\WyuczygTWM2OD15IH7N MYSxO|EzOzh{MR?=
Sf9 cells NU\ORnZLTnWwY4Tpc44h[XO|YYm= Mn7oTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDjfYNtcW5iQT;DSGszKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MUKgcm0> MofLNVc6ODR|Nk[=
LNCaP human prostate carcinoma cell M3LtXnBzd2yrZnXyZZRqd25iYYPzZZk> NGLjboZKdmirYnn0bY9vKG:oIFzOR4FRKGi3bXHuJJBzd3O2YYTlJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44> MXKxNlE6ODNzMx?=
HCT116/VP35 human colon carcinoma cell NH\jOVRRem:uaX\ldoF1cW:wIHHzd4F6 NWTiN5lTUW6qaXLpeIlwdiCxZjDIR3QyOTZxVmCzOUBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTF5IH7N MYqxNlE6ODNzMx?=
HCT116 human colon carcinoma cell NX;LU5J7WHKxbHnm[ZJifGmxbjDhd5NigQ>? MnzzTY5pcWKrdHnvckBw\iCKQ2SxNVYhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1zODDuUS=> MVSxNlE6ODNzMx?=
HCT116/VM46 human colon carcinoma cell MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NVTpUoM{UW6qaXLpeIlwdiCxZjDIR3QyOTZxVl20OkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTJzIH7N NWPQfnFYOTJzOUCzNVM>
human A2780 cells NHzoZ3FEgXSxdH;4bYPDqGG|c3H5 Mk\1NlQhcA>? M2j0XWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUC9NlMhdk1? NGX1SIUzOzNyMUe2Oy=>
MCF7 cells MmGyVJJwdGmoZYLheIlwdiCjc4PhfS=> MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOsJGlEPTB;Mk[gcm0> MlLPNVcyOjN6MkG=
human MRC5 cells MnuzR5l1d3SxeHnjxsBie3OjeR?= MUG3NkBp MoTaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUK4JI5O MYSyN|MxOTd4Nx?=
human A2780 cells MnXxR5l1d3SxeHnjxsBie3OjeR?= MlLXO|IhcA>? NIjrdnpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVI6KG6P M1\FR|I{OzBzN{[3
human A2780 cells MnnyR5l1d3SxeHnjxsBie3OjeR?= NVzHZmZyPDhiaB?= MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUOxJI5O NYDtVoVPOjN|MEG3Olc>
A2780/DDP-R human ovarian carcinoma cell MULQdo9tcW[ncnH0bY9vKGG|c3H5 NYHpUog2UW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;M{igcm0> NYnBOYhTOTJzOUCzNVM>
human MRC5 cells NWG3PXFUS3m2b4TvfIlkyqCjc4PhfS=> M3;BU|Q5KGh? MoTYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUO5JI5O MVWyN|MxOTd4Nx?=
ABAE human fibroblast cell MVXQdo9tcW[ncnH0bY9vKGG|c3H5 MWfJcohq[mm2aX;uJI9nKEGEQVWgbJVu[W5iZnnido9jdGG|dDDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NEWgcm0> MmjRNVIyQTB|MUO=
HL60 human leukemia cell NYfxdXVbWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYDLeVdnUW6qaXLpeIlwdiCxZjDIUFYxKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME20OkBvVQ>? M4P2flEzOTlyM{Gz
human MRC5 cells M2LP[GN6fG:2b4jpZ:Kh[XO|YYm= MVqyOEBp NYDkUGFYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVQ6KG6P MX:yN|MxOTd4Nx?=
Hs 27 human fibroblast cell NULxdFc6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGfCbXRKdmirYnn0bY9vKG:oIFjzJFI4KGi3bXHuJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVUyKG6P M1eyNFEzOTlyM{Gz
CCRF-CEM human leukemia cell MYLQdo9tcW[ncnH0bY9vKGG|c3H5 MWLJcohq[mm2aX;uJI9nKEOFUl[tR2VOKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21NkBvVQ>? NYPmbohnOTJzOUCzNVM>
OVCAR-3 human ovarian carcinoma cell Mk[wVJJwdGmoZYLheIlwdiCjc4PhfS=> NWjjU4ExUW6qaXLpeIlwdiCxZjDPWmNCWi1|IHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02PCCwTR?= MXWxNlE6ODNzMx?=
A2780/DDP-S human ovarian carcinoma cell NHf5ZXRRem:uaX\ldoF1cW:wIHHzd4F6 M4PyWmlvcGmkaYTpc44hd2ZiQUK3PFAwTESSLWOgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTV4IH7N MYOxNlE6ODNzMx?=
human HMEC1 cells M4XsO2N6fG:2b4jpZ:Kh[XO|YYm= MWGyOEBp NFv5c2dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVYyKG6P M2rL[FI{OzBzN{[3
human HMEC1 cells Ml\2R5l1d3SxeHnjxsBie3OjeR?= NX3QTJh7PDhiaB?= NVTiWnZLS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE2HQ{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF03OiCwTR?= M1ToWlI{OzBzN{[3
A2780/TAX-S human ovarian carcinoma cell NU[2e3IzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoLUTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PjVibl2= NF3RW|gyOjF7MEOxNy=>
LS174T human colon carcinoma cell M1H6OHBzd2yrZnXyZZRqd25iYYPzZZk> NYr5N4dNUW6qaXLpeIlwdiCxZjDMV|E4PFRiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OUBvVQ>? NXza[YdLOTJzOUCzNVM>
MCF-7 human breast carcinoma cell NWfpbmF[WHKxbHnm[ZJifGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKE2FRj23JIh2dWGwIHLy[YF{fCClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N MY[xNlE6ODNzMx?=
human HMEC1 cells NIOwT|VEgXSxdH;4bYPDqGG|c3H5 MlvVO|IhcA>? M4HPfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhOTUNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9OlYhdk1? NFLYXWozOzNyMUe2Oy=>
PC3 human prostate carcinoma cell NUf3XoRUWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHnUVnZKdmirYnn0bY9vKG:oIGDDN{BpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MXqxNlE6ODNzMx?=
human A2780 cell line MVLQdo9tcW[ncnH0bY9vKGG|c3H5 NWXiWFdQPzJiaB?= NED0WG9CdnSrcILvcIln\XKjdHn2[UBm\m[nY4SgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgbY4h[SC5aH;s[UBk\WyuIEeyJIhzKGO7dH;0c5hq[2m2eTDhd5NigSxiSVO1NF04OSCwTR?= MmK1NVUxOjd6NkO=
human ovarian (A2780) cancer cell NWPEdpdUS3m2b4TvfIlkyqCjc4PhfS=> MkPWR5l1d3SxeHnjJIVn\mWldDDvckBpfW2jbjDveoFzcWGwIDjBNlc5OCliY3HuZ4VzKGOnbHygcIlv\SxiSVO1NF04OSCwTR?= NV2ybIJIOTVzMkW5O|E>
MLF mouse lung fibroblast cell MWfQdo9tcW[ncnH0bY9vKGG|c3H5 NVf0fZd7UW6qaXLpeIlwdiCxZjDNUGYhdW:3c3WgcJVv\yCoaXLyc4Jt[XO2IHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15MjDuUS=> M1nXPFEzOTlyM{Gz
human NCI60 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MYi3NkBp NUHzU3U1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF04PC55IH7N NX;JSVNoOjFyOEC3NFM>
LX-1 human lung carcinoma NETOUWRRem:uaX\ldoF1cW:wIHHzd4F6 MXfJcohq[mm2aX;uJI9nKEy[LUGgbJVu[W5ibIXu[{Bk[XKlaX7vcYEheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> MorhNVIyQTB|MUO=
A431 human squamous cell NUDGNJhDWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P MlK4NVIyQTB|MUO=
SKBR-3 human breast carcinoma cell M{nUSXBzd2yrZnXyZZRqd25iYYPzZZk> NE\xZoJKdmirYnn0bY9vKG:oIGPLRnIuOyCqdX3hckBjemWjc4SgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME23O{BvVQ>? MoeyNVIyQTB|MUO=
A2780/TAX-R human ovarian carcinoma cell NIfTbo1Rem:uaX\ldoF1cW:wIHHzd4F6 M17LdmlvcGmkaYTpc44hd2ZiQUK3PFAwXEG[LWKgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTd6IH7N NVvmRZNCOTJzOUCzNVM>
M109 mouse lung carcinoma cell MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MoPPTY5pcWKrdHnvckBw\iCPMUC5JI1wfXOnIHz1coch[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF05OCCwTR?= NVKzdZZHOTJzOUCzNVM>
CACO-2 human colon carcinoma cell MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NEW0ZY5KdmirYnn0bY9vKG:oIFPBR28uOiCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUi2JI5O M32xeFEzOTlyM{Gz
A549 human lung carcinoma cell MnLzVJJwdGmoZYLheIlwdiCjc4PhfS=> NGHIcplKdmirYnn0bY9vKG:oIFG1OFkhcHWvYX6gcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTl4IH7N M2fmcFEzOTlyM{Gz
MIP human colon carcinoma cell NHTZfWpHfW6ldHnvckBie3OjeR?= NELURXhKdmirYnn0bY9vKG:oIF3JVEBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBtcW6nLDDJR|UxRTBwMUKg{txO MXqxNlE6ODNzMx?=
K562 human leukemia cell NF:4WHdRem:uaX\ldoF1cW:wIHHzd4F6 MX;Jcohq[mm2aX;uJI9nKEt3NkKgbJVu[W5ibHX1b4VucWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTBwMUOg{txO M{\qW|EzOTlyM{Gz
MCF-7 tumor cell MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NWLBNYtOUW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> NXjKXIdOOTB6NEOyNVE>
human NCI60 cells M2fqNXBzd2yrZnXyZZRqd25iYYPzZZk> MUW3NkBp MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FSU[wJINmdGy|IHHzd4V{e2WmIHHzJIxmfGijbDDl[oZm[3RiYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGxEPTB;MD65NFQh|ryP NE[0OXEzOTB6MEewNy=>
PC3 cell MoXJSpVv[3Srb36gZZN{[Xl? NUTBOWV[UW6qaXLpeIlwdiCxZjDQR|Mh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTFyIN88US=> NEnH[3QyOTB4M{[wPS=>
HCT116 cell MW\GeY5kfGmxbjDhd5NigQ>? MlfDTY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> MnnJNVExPjN4MEm=
A2780 cell MXLGeY5kfGmxbjDhd5NigQ>? M33xXmlvcGmkaYTpc44hd2ZiQUK3PFAh[2WubDDjcI9vd2enbnnjJIF{e2G778{MJGlEPTB;MUWg{txO NHW2Z4QyOTB4M{[wPS=>
Mia PaCa-2 cell NXOyc5k{TnWwY4Tpc44h[XO|YYm= MXXJcohq[mm2aX;uJI9nKE2rYTDQZWNiNTJiY3XscEBkdG:wb3flcolkKGG|c3H5MEBKSzVyPUO2JO69VQ>? NGHlW2EyOTB4M{[wPS=>
human A2780 cells M1TvU2Z2dmO2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGOmaz3t[YRq[XSnZDDOVG0heGixc4Doc5J6dGG2aX;uJIF1KHSqckG5PUBqdiCqdX3hckBCOjd6MDDj[Yxtew>? MVuxPFQ3QThyOR?=
human A2780 cells M3rhfWZ2dmO2aX;uJIF{e2G7 M3zWXVI1KGh? MYPJcohq[mm2aX;uJI9nKGOmaz3t[YRq[XSnZDDSZkBxcG:|cHjvdplt[XSrb36gZZQhfGi{OEKxJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFI1KGi{cx?= MnLrNVg1Pjl6MEm=

... 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(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 (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 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
NCT00003620 Completed Drug: alvocidib|Other: laboratory biomarker analysis B-cell Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia National Cancer Institute (NCI) June 1999 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID