Flavopiridol (Alvocidib)

Catalog No.S1230 Synonyms: NSC 649890 HCl,HMR-1275

Flavopiridol (Alvocidib) Chemical Structure

Molecular Weight(MW): 401.84

Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

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Cited by 25 Publications

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Choose Selective CDK Inhibitors

Biological Activity

Description Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
Features First CDK inhibitor to be used in human clinical trials.
Targets
CDK9 [8]
(Cell-free assay)
CDK1 [8]
(Cell-free assay)
CDK4 [9]
(Cell-free assay)
CDK2 [8]
(Cell-free assay)
CDK6 [9]
(Cell-free assay)
20 nM 30 nM 20-40 nM 40 nM 60 nM
In vitro

Flavopiridol displays less activity against unrelated kinases such as MAP, PAK, PKC, and EGFR with IC50 of >14 μM. Flavopiridol significantly inhibits the colony growth of HCT116, A2780, PC3, and Mia PaCa-2 cells with IC50 of 13 nM, 15 nM, 10 nM and 36 nM, respecitively. [1] Flavopiridol also potently inhibits the activity of Glycogen synthase kinase-3 (GSK-3) with an IC50 of 280 nm. [2] Compared with other CDKs, Flavopiridol inhibits the activity of CDK7 less potently with IC50 of 875 nM. Flavopiridol (0.5 μM) inhibits both pSer807/811 Rb and pThr199 NPM, whereas mild changes are observed at pThr821 Rb. Flavopiridol also decreases the overall RNA polymerase II level, as well as the phosphorylation of RNA polymerase II on the CTD repeats at Ser2 Ser5. [3] As a broad spectrum CDK inhibitor, Flavopiridol can inhibit cell cycle progression in either G1 or G2. Flavopiridol (0.3 μM) induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. [4] Flavopiridol exhibits potent cytotoxicity against a wide variety of tumor cell lines with IC50 values ranging form 16 nM for LNCAP to 130 nM for K562. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ID8 cells NGrjcZZRem:uaX\ldoF1cW:wIHHzd4F6 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFnEPEBk\WyuczygTWM2OD15IH7N MYixO|EzOzh{MR?=
Sf9 cells MYLGeY5kfGmxbjDhd5NigQ>? MkG1TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDjfYNtcW5iQT;DSGszKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MUKgcm0> M2i0OFE4QTB2M{[2
LNCaP human prostate carcinoma cell Ml\BVJJwdGmoZYLheIlwdiCjc4PhfS=> MVXJcohq[mm2aX;uJI9nKEyQQ3HQJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36= M{G3T|EzOTlyM{Gz
HCT116/VP35 human colon carcinoma cell MkHOVJJwdGmoZYLheIlwdiCjc4PhfS=> NGDwWWhKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= Mln5NVIyQTB|MUO=
HCT116 human colon carcinoma cell MkTuVJJwdGmoZYLheIlwdiCjc4PhfS=> NWfp[YQyUW6qaXLpeIlwdiCxZjDIR3QyOTZiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2xPEBvVQ>? MkjqNVIyQTB|MUO=
HCT116/VM46 human colon carcinoma cell MVTQdo9tcW[ncnH0bY9vKGG|c3H5 M1LBcmlvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= MnjrNVIyQTB|MUO=
human A2780 cells NX[wclF5S3m2b4TvfIlkyqCjc4PhfS=> M{mwRlI1KGh? NV7UeHl{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zOyCwTR?= NY\GUZRROjN|MEG3Olc>
MCF7 cells MnzlVJJwdGmoZYLheIlwdiCjc4PhfS=> NIPOeIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JG1ETjdiY3XscJMtKEmFNUC9NlYhdk1? NYLTdXozOTdzMkO4NlE>
human MRC5 cells MnnmR5l1d3SxeHnjxsBie3OjeR?= MXS3NkBp NUTuWpF7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVI5KG6P NGSyb3IzOzNyMUe2Oy=>
human A2780 cells MmPGR5l1d3SxeHnjxsBie3OjeR?= Mo\GO|IhcA>? M{nnbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlkhdk1? NGK3PWkzOzNyMUe2Oy=>
human A2780 cells MVfDfZRwfG:6aXRCpIF{e2G7 NHr5e|E1QCCq M1zycmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEeLNUC9N|Ehdk1? M4\qUFI{OzBzN{[3
A2780/DDP-R human ovarian carcinoma cell NFXoZlBRem:uaX\ldoF1cW:wIHHzd4F6 NFLSOo5KdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3SJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1|ODDuUS=> MW[xNlE6ODNzMx?=
human MRC5 cells MVjDfZRwfG:6aXRCpIF{e2G7 MnvHOFghcA>? M3X6NWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2zPUBvVQ>? Mn3KNlM{ODF5Nke=
ABAE human fibroblast cell M1jHNHBzd2yrZnXyZZRqd25iYYPzZZk> NFXoR2tKdmirYnn0bY9vKG:oIFHCRWUhcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OFUhdk1? NXTqS|BOOTJzOUCzNVM>
HL60 human leukemia cell MWTQdo9tcW[ncnH0bY9vKGG|c3H5 MljrTY5pcWKrdHnvckBw\iCKTE[wJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD12NjDuUS=> NH[2eWsyOjF7MEOxNy=>
human MRC5 cells M4XqeWN6fG:2b4jpZ:Kh[XO|YYm= NEf2[W0zPCCq MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;NEmgcm0> NHHXeYozOzNyMUe2Oy=>
Hs 27 human fibroblast cell MoC0VJJwdGmoZYLheIlwdiCjc4PhfS=> NVTzWXRXUW6qaXLpeIlwdiCxZjDId{AzPyCqdX3hckBncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OSCwTR?= MmnBNVIyQTB|MUO=
CCRF-CEM human leukemia cell NIW5fWRRem:uaX\ldoF1cW:wIHHzd4F6 MXzJcohq[mm2aX;uJI9nKEOFUl[tR2VOKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21NkBvVQ>? Mki2NVIyQTB|MUO=
OVCAR-3 human ovarian carcinoma cell NY\0bm5yWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nyWGlvcGmkaYTpc44hd2ZiT2\DRXIuOyCqdX3hckBwfmG{aXHuJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVQhdk1? MX:xNlE6ODNzMx?=
A2780/DDP-S human ovarian carcinoma cell NVjQVGlRWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkfzTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTZibl2= NFu4b4UyOjF7MEOxNy=>
human HMEC1 cells M2PnUWN6fG:2b4jpZ:Kh[XO|YYm= MoTaNlQhcA>? M4\aeGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhOTUNzIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUC9OlEhdk1? NWDjblNtOjN|MEG3Olc>
human HMEC1 cells NUL6cVRCS3m2b4TvfIlkyqCjc4PhfS=> NFT3TWo1QCCq MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[yJI5O MUOyN|MxOTd4Nx?=
A2780/TAX-S human ovarian carcinoma cell MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 MofBTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PjVibl2= MnntNVIyQTB|MUO=
LS174T human colon carcinoma cell M1:zWHBzd2yrZnXyZZRqd25iYYPzZZk> M4fXZ2lvcGmkaYTpc44hd2ZiTGOxO|RVKGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NkWgcm0> NXXXTHNtOTJzOUCzNVM>
MCF-7 human breast carcinoma cell M2H2SHBzd2yrZnXyZZRqd25iYYPzZZk> NHfGUZdKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MmLONVIyQTB|MUO=
human HMEC1 cells NGjhUVdEgXSxdH;4bYPDqGG|c3H5 MoDwO|IhcA>? M3n6PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhOTUNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9OlYhdk1? MkXFNlM{ODF5Nke=
PC3 human prostate carcinoma cell MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NXP0U|dsUW6qaXLpeIlwdiCxZjDQR|MhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME22OkBvVQ>? MWmxNlE6ODNzMx?=
human A2780 cell line NEmz[ZZRem:uaX\ldoF1cW:wIHHzd4F6 NXvUUFNyPzJiaB?= MnK1RY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9O|Ehdk1? NULEWWZ1OTVyMke4OlM>
human ovarian (A2780) cancer cell NF3hVnJEgXSxdH;4bYPDqGG|c3H5 NXnTfo1oS3m2b4TvfIlkKGWoZnXjeEBwdiCqdX3hckBwfmG{aXHuJEhCOjd6MDmgZ4Fv[2W{IHPlcIwhdGmwZTygTWM2OD15MTDuUS=> MYGxOVEzPTl5MR?=
MLF mouse lung fibroblast cell MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 Mn7OTY5pcWKrdHnvckBw\iCPTF[gcY92e2VibIXu[{BncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04OiCwTR?= MXOxNlE6ODNzMx?=
human NCI60 cells NVnaVXNEWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYe3NkBp MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FSU[wJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUe0Mlchdk1? M{XnPFIyODhyN{Cz
LX-1 human lung carcinoma NEXCXZJRem:uaX\ldoF1cW:wIHHzd4F6 M2jrNWlvcGmkaYTpc44hd2ZiTGitNUBpfW2jbjDseY5oKGOjcnPpco9u[SCycn;sbYZmemG2aX;uMEBKSzVyPUe1JI5O MornNVIyQTB|MUO=
A431 human squamous cell NF3pNoRRem:uaX\ldoF1cW:wIHHzd4F6 MlvJTY5pcWKrdHnvckBw\iCDNEOxJIh2dWGwIIPxeYFud3W|IHPlcIwh[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04PSCwTR?= NGfGZ3MyOjF7MEOxNy=>
SKBR-3 human breast carcinoma cell M3S1S3Bzd2yrZnXyZZRqd25iYYPzZZk> M{PiSGlvcGmkaYTpc44hd2ZiU1vCVk0{KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUe3JI5O MVKxNlE6ODNzMx?=
A2780/TAX-R human ovarian carcinoma cell MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MXLJcohq[mm2aX;uJI9nKEF{N{iwM3RCYC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04QCCwTR?= MWCxNlE6ODNzMx?=
M109 mouse lung carcinoma cell Ml3sVJJwdGmoZYLheIlwdiCjc4PhfS=> NETyU4JKdmirYnn0bY9vKG:oIF2xNFkhdW:3c3WgcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRThyIH7N MkSxNVIyQTB|MUO=
CACO-2 human colon carcinoma cell NYXkbGMxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFjIV49KdmirYnn0bY9vKG:oIFPBR28uOiCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUi2JI5O MVixNlE6ODNzMx?=
A549 human lung carcinoma cell NUOyW2JSWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIfONlFKdmirYnn0bY9vKG:oIFG1OFkhcHWvYX6gcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTl4IH7N M3P1UlEzOTlyM{Gz
MIP human colon carcinoma cell NVjNe|R7TnWwY4Tpc44h[XO|YYm= MnqyTY5pcWKrdHnvckBw\iCPSWCgbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygcIlv\SxiSVO1NF0xNjF{IN88US=> NF3Hb3kyOjF7MEOxNy=>
K562 human leukemia cell M4\zfHBzd2yrZnXyZZRqd25iYYPzZZk> NH6xeGRKdmirYnn0bY9vKG:oIFu1OlIhcHWvYX6gcIV2c2WvaXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUCuNVMh|ryP NVm5Zo95OTJzOUCzNVM>
MCF-7 tumor cell M{K2bnBzd2yrZnXyZZRqd25iYYPzZZk> M4fsXmlvcGmkaYTpc44hd2ZiTVPGMVchfHWvb4KgZ4VtdCCycn;sbYZmemG2aX;u M17uflExQDR|MkGx
human NCI60 cells MnrEVJJwdGmoZYLheIlwdiCjc4PhfS=> MWO3NkBp Mmj6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1m2NEBk\WyuczDhd5Nme3OnZDDhd{Bt\XSqYXyg[YZn\WO2IHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBNSzVyPUCuPVA1KM7:TR?= NXHzZlJyOjFyOEC3NFM>
PC3 cell NVHpOFBGTnWwY4Tpc44h[XO|YYm= M4T3cWlvcGmkaYTpc44hd2ZiUFOzJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0yOCEQvF2= M3ftXVEyODZ|NkC5
HCT116 cell NWO5bm9vTnWwY4Tpc44h[XO|YYm= MlG0TY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> Mn\RNVExPjN4MEm=
A2780 cell MYXGeY5kfGmxbjDhd5NigQ>? M37PZmlvcGmkaYTpc44hd2ZiQUK3PFAh[2WubDDjcI9vd2enbnnjJIF{e2G778{MJGlEPTB;MUWg{txO Mnu0NVExPjN4MEm=
Mia PaCa-2 cell NYTyXYhVTnWwY4Tpc44h[XO|YYm= NYr0XnllUW6qaXLpeIlwdiCxZjDNbYEhWGGFYT2yJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0{PiEQvF2= NIjhd3QyOTB4M{[wPS=>
human A2780 cells MVjGeY5kfGmxbjDhd5NigQ>? NX7KNVdSUW6qaXLpeIlwdiCxZjDj[IsudWWmaXH0[YQhVlCPIIDoc5NxcG:{eXzheIlwdiCjdDD0bJIyQTliaX6gbJVu[W5iQUK3PFAh[2WubIO= NH\SVm0yQDR4OUiwPS=>
human A2780 cells NX;GVFJXTnWwY4Tpc44h[XO|YYm= M3XLTVI1KGh? NWPSSWI2UW6qaXLpeIlwdiCxZjDj[IsudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IITodlgzOSCrbjDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB{NDDodpM> NWX5PYFtOTh2Nkm4NFk>

... Click to View More Cell Line Experimental Data

In vivo Administration of Flavopiridol at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, resulting in %T/C value of 110, and active against the human A2780 ovarian carcinoma implanted sc in nude mice, producing 1.5 log cell kill (LCK). [5] Flavopiridol treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. [6] In the p21-intact Hct116 xenografts in nude mice, administration of CPT-11 (100 mg/kg) followed by Flavopiridol (3 mg/kg) 7 and 16 hours later significantly inhibits tumor regression by 86% and 82%, respectively, displaying >2 fold inhibition compared with CPT-11 alone by 40 %. The combination produces ~30% complete response rate (CR) in contrast to CPT-11 alone where no CR is found. [7]

Protocol

Kinase Assay:

[1]

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CDK kinase assay:

For CDK1/cyclin B1 kinase assay, kinase reactions consist of 100 ng of baculovirus expressed GST-CDK1/cyclin B1 (human) complex, 1 μg histone HI, 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT). For CDK2/cyclin E kinase assay, kinase reactions consist of 5 ng of baculovirus expressed GST-CDK2/cyclin E (human) complex, 0.5 μg GST-RB fusion protein (amino acids 776-928 of retinoblastoma protein), 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT). For CDK4/cyclin D1 kinase assay, kinase reactions consist of 150 ng of baculovirus expressed GST-CDK4/cyclin D1 (human), 280 ng of Stag-cyclin D1, 0.5 μg GST-RB fusion protein (amino acids 776-928 of retinoblastoma protein), 0.2 μCi [γ-33P]ATP, 25 μM ATP in 50 μL kinase buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT). Reactions are incubated for 45 minutes for CDK1 and CDK2, or 1 hour for CDK4 at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration 15%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Flavopiridol is dissolved at 10 mM in dimethylformamide (DMF) and evaluated at six concentrations, each in triplicate. The final concentration of DMF in the assay = 2%. IC50 values are derived by nonlinear regression analysis and have a coefficient of variance = 16%. To assay Flavopiridol activity on CDK6, a filter-binding assay is established. The following are combined in the reaction mixture: 2 μL of CDK6 (0.7 mg/μL), 5 μL of histone H1 (6 mg/mL), 14 μL of kinase buffer (60 mM β-glycerophosphate, 30 mM p-nitrophenyl phosphate, 25 mM MOPS (pH 7.0), 5 mM EGTA, 15 mM MgCl2, 1 mM DTT, 0.1 mM Na-vanadate), 3 μL of increasing concentrations of Flavopiridol diluted in 50% DMSO, and 6 μL of 33P-ATP (1 mCi/mL) in nonradioactive ATP at 90 μM concentration (final concentration: 15 μM). The assay is initiated by the addition of 33P-ATP. The reaction is incubated for 20 minutes at 30°C. A 25 μL aliquot of the supernatant is then spotted onto Whatman P81 phosphocellulose paper. Filters are washed 5 times with 1% phosphoric acid solution. Wet filters are counted in the presence of 1 mL of scintillation fluid. Cdk9 activity is measured using 50 nM of recombinant Cdk9/cyclin T in 50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 3 μM Na3VO4, 150 μM RNA polymerase CDT peptide and 80 μM ATP. Cdk7 assay is performed in the same buffer using 37 nM of purified kinase in the presence of 200 μM ATP and 10 μM myelin binding protein as a substrate. The potency of Flavopiridol toward CDK9 and CDK7 is determined using either a strong anion exchanger (Dowex 1-X8 resin, formate form)-based assay or a scintillation proximity assay. IC50 values are calculated from the dose-response curves.
Cell Research:

[5]

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  • Cell lines: MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562 cells and et al.
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Flavopiridol for 72 hours at which time the tetrazolium dye, MTS in combination with phenazine methosulfate, is added. After 3 hours, the absorbency is measured at 492 nm, which is proportional to the number of viable cells. The results are expressed as IC50 values. For cell Cycle analysis, cells are fixed in paraformaldehyde and ethanol, washed, resuspended in staining solution of TdT enzyme and FITC-dUTP, washed, stained with PI following RNase treatment, and then analyzed by flow cytometry.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: Female Balb/c×DBA/2J F1 mice inoculated ip with P388 ascites leukemic cells, and Balb/c nu/nu nude mice subcutaneous implanted with A2780, Br-cycE, or A431 cells
  • Formulation: Dissolved in a mixture of Cremophor/ethanol (50:50), and diluted in water
  • Dosages: ~7.5 mg/kg/day
  • Administration: Injection i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (37.32 mM)
Ethanol 8 mg/mL (19.9 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2.5mg/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 401.84
Formula

C21H20ClNO5

CAS No. 146426-40-6
Storage powder
in solvent
Synonyms NSC 649890 HCl,HMR-1275

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
NCT03593915 Recruiting Myelodysplastic Syndromes (MDS) Tolero Pharmaceuticals Inc. August 29 2018 Phase 1|Phase 2
NCT03593915 Recruiting Myelodysplastic Syndromes (MDS) Tolero Pharmaceuticals Inc. August 29 2018 Phase 1|Phase 2
NCT03563560 Recruiting Acute Myeloid Leukemia Sumitomo Dainippon Pharma Co. Ltd. May 15 2018 Phase 1
NCT03441555 Recruiting Acute Myeloid Leukemia (AML) AbbVie|Tolero Pharmaceuticals Inc. May 30 2018 Phase 1
NCT03563560 Recruiting Acute Myeloid Leukemia Sumitomo Dainippon Pharma Co. Ltd. May 15 2018 Phase 1
NCT03441555 Recruiting Acute Myeloid Leukemia (AML) AbbVie|Tolero Pharmaceuticals Inc. May 30 2018 Phase 1

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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