Flavopiridol (Alvocidib)

For research use only. Not for use in humans.

製品コードS1230 別名:NSC 649890 HCl,HMR-1275

Flavopiridol (Alvocidib)化学構造

分子量(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. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.

サイズ 価格(税別) 在庫  
JPY 10300 あり
JPY 30200 あり
JPY 96600 あり
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バルク問合せ

文献中Selleckの製品使用例(58)

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明 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. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
特性 First CDK inhibitor to be used in human clinical trials.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ID8 cells NWG5S5p5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M{TEOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTWQ5KGOnbHzzMEBKSzVyPUegcm0> NEjPOpQyPzF{M{iyNS=>
Sf9 cells MUjGeY5kfGmxbjDhd5NigQ>? MmLlTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDjfYNtcW5iQT;DSGszKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MUKgcm0> NETIfZIyPzlyNEO2Oi=>
LNCaP human prostate carcinoma cell MXXQdo9tcW[ncnH0bY9vKGG|c3H5 MVfJcohq[mm2aX;uJI9nKEyQQ3HQJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36= M1jZW|EzOTlyM{Gz
HCT116/VP35 human colon carcinoma cell NYG2fFBtWHKxbHnm[ZJifGmxbjDhd5NigQ>? NI\EUotKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= NHTSemoyOjF7MEOxNy=>
HCT116 human colon carcinoma cell NXT3co1JWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkPmTY5pcWKrdHnvckBw\iCKQ2SxNVYhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1zODDuUS=> NGrsd2syOjF7MEOxNy=>
HCT116/VM46 human colon carcinoma cell M1PVW3Bzd2yrZnXyZZRqd25iYYPzZZk> M13EZ2lvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= MVSxNlE6ODNzMx?=
human A2780 cells MnnFR5l1d3SxeHnjxsBie3OjeR?= M4LpUlI1KGh? M4P1eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUC9NlMhdk1? NHPPSpUzOzNyMUe2Oy=>
MCF7 cells NFr5NFNRem:uaX\ldoF1cW:wIHHzd4F6 M3;CO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWNHPyClZXzsd{whUUN3ME2yOkBvVQ>? M37GblE4OTJ|OEKx
human MRC5 cells MmjXR5l1d3SxeHnjxsBie3OjeR?= MYm3NkBp Ml2xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUK4JI5O Mlz0NlM{ODF5Nke=
human A2780 cells M33uTGN6fG:2b4jpZ:Kh[XO|YYm= NWnDSmoxPzJiaB?= NXj0elQxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zQSCwTR?= Mki1NlM{ODF5Nke=
human A2780 cells MXrDfZRwfG:6aXRCpIF{e2G7 NVzGWJM{PDhiaB?= M1LTZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEeLNUC9N|Ehdk1? M1TocVI{OzBzN{[3
A2780/DDP-R human ovarian carcinoma cell NIjodnFRem:uaX\ldoF1cW:wIHHzd4F6 NEm2OHVKdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3SJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1|ODDuUS=> M1WwPFEzOTlyM{Gz
human MRC5 cells MVXDfZRwfG:6aXRCpIF{e2G7 NGTmb5Y1QCCq NXfhZXlQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVM6KG6P NHrH[3ozOzNyMUe2Oy=>
ABAE human fibroblast cell NITySWRRem:uaX\ldoF1cW:wIHHzd4F6 NWfRSnl5UW6qaXLpeIlwdiCxZjDBRmFGKGi3bXHuJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVQ2KG6P M{Hr[VEzOTlyM{Gz
HL60 human leukemia cell M4qxWnBzd2yrZnXyZZRqd25iYYPzZZk> MXXJcohq[mm2aX;uJI9nKEiONkCgbJVu[W5ibHX1b4VucWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTR4IH7N NFzQVlgyOjF7MEOxNy=>
human MRC5 cells NXPhWllGS3m2b4TvfIlkyqCjc4PhfS=> M1Wxc|I1KGh? NFHzUGVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUC9OFkhdk1? NXzo[GhxOjN|MEG3Olc>
Hs 27 human fibroblast cell NX;lWIl6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2DoPGlvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? NYT3VY1GOTJzOUCzNVM>
CCRF-CEM human leukemia cell Mlu0VJJwdGmoZYLheIlwdiCjc4PhfS=> NHfMXYZKdmirYnn0bY9vKG:oIFPDVmYuS0WPIHj1cYFvKGyndXvlcYliKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OiCwTR?= NELhS28yOjF7MEOxNy=>
OVCAR-3 human ovarian carcinoma cell Mnf3VJJwdGmoZYLheIlwdiCjc4PhfS=> M1rMdWlvcGmkaYTpc44hd2ZiT2\DRXIuOyCqdX3hckBwfmG{aXHuJINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVQhdk1? M3nnbVEzOTlyM{Gz
A2780/DDP-S human ovarian carcinoma cell MlnZVJJwdGmoZYLheIlwdiCjc4PhfS=> NWDWenRQUW6qaXLpeIlwdiCxZjDBNlc5OC:GRGCtV{BpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NU[gcm0> MoS4NVIyQTB|MUO=
human HMEC1 cells NGrMc3hEgXSxdH;4bYPDqGG|c3H5 M2LMNFI1KGh? MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[xJI5O NWDCR|RzOjN|MEG3Olc>
human HMEC1 cells M2\TVGN6fG:2b4jpZ:Kh[XO|YYm= MW[0PEBp Ml;nR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTG1GSzFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME22NkBvVQ>? NGfST|EzOzNyMUe2Oy=>
A2780/TAX-S human ovarian carcinoma cell Mm\vVJJwdGmoZYLheIlwdiCjc4PhfS=> MkjrTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PjVibl2= MWmxNlE6ODNzMx?=
LS174T human colon carcinoma cell Mm\TVJJwdGmoZYLheIlwdiCjc4PhfS=> NH34eFFKdmirYnn0bY9vKG:oIFzTNVc1XCCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[1JI5O NYLKeFRMOTJzOUCzNVM>
MCF-7 human breast carcinoma cell MnrqVJJwdGmoZYLheIlwdiCjc4PhfS=> Mon2TY5pcWKrdHnvckBw\iCPQ1[tO{BpfW2jbjDidoVie3RiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NjDuUS=> MV[xNlE6ODNzMx?=
human HMEC1 cells NWG5OJVVS3m2b4TvfIlkyqCjc4PhfS=> NXPYWZJ4PzJiaB?= NGSyOYxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVUWFMTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVY3KG6P M3GxO|I{OzBzN{[3
PC3 human prostate carcinoma cell MkfGVJJwdGmoZYLheIlwdiCjc4PhfS=> MX3Jcohq[mm2aX;uJI9nKFCFMzDoeY1idiCycn;zeIF1\SClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N NWTUVJRVOTJzOUCzNVM>
human A2780 cell line MUjQdo9tcW[ncnH0bY9vKGG|c3H5 MUW3NkBp MmjSRY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9O|Ehdk1? M4rSclE2ODJ5OE[z
human ovarian (A2780) cancer cell MmjRR5l1d3SxeHnjxsBie3OjeR?= NIHkTVREgXSxdH;4bYMh\W[oZXP0JI9vKGi3bXHuJI93[XKrYX6gLGEzPzhyKTDjZY5k\XJiY3XscEBtcW6nLDDJR|UxRTdzIH7N M3vZS|E2OTJ3OUex
MLF mouse lung fibroblast cell NWjh[VB3WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mo\RTY5pcWKrdHnvckBw\iCPTF[gcY92e2VibIXu[{BncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04OiCwTR?= MnGxNVIyQTB|MUO=
human NCI60 cells NFzJUGtRem:uaX\ldoF1cW:wIHHzd4F6 NH7iV4g4OiCq MmntRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1m2NEBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME23OE44KG6P NI\ibXozOTB6MEewNy=>
LX-1 human lung carcinoma M{LPN3Bzd2yrZnXyZZRqd25iYYPzZZk> MYjJcohq[mm2aX;uJI9nKEy[LUGgbJVu[W5ibIXu[{Bk[XKlaX7vcYEheHKxbHnm[ZJifGmxbjygTWM2OD15NTDuUS=> MXKxNlE6ODNzMx?=
A431 human squamous cell MmHoVJJwdGmoZYLheIlwdiCjc4PhfS=> MVvJcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P NHfp[WMyOjF7MEOxNy=>
SKBR-3 human breast carcinoma cell MmP1VJJwdGmoZYLheIlwdiCjc4PhfS=> MX;Jcohq[mm2aX;uJI9nKFONQmKtN{BpfW2jbjDidoVie3RiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15NzDuUS=> MlnSNVIyQTB|MUO=
A2780/TAX-R human ovarian carcinoma cell NFPGfZBRem:uaX\ldoF1cW:wIHHzd4F6 MmfXTY5pcWKrdHnvckBw\iCDMke4NE9VSVhvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Pzhibl2= NI\FbVgyOjF7MEOxNy=>
M109 mouse lung carcinoma cell MkDZVJJwdGmoZYLheIlwdiCjc4PhfS=> MWjJcohq[mm2aX;uJI9nKE1zMEmgcY92e2VibIXu[{Bk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVgxKG6P NFq4TG0yOjF7MEOxNy=>
CACO-2 human colon carcinoma cell NUjiSHpHWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWr0T2NGUW6qaXLpeIlwdiCxZjDDRWNQNTJiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME24OkBvVQ>? NV\5d|ZrOTJzOUCzNVM>
A549 human lung carcinoma cell MWTQdo9tcW[ncnH0bY9vKGG|c3H5 Mn3NTY5pcWKrdHnvckBw\iCDNUS5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF06PiCwTR?= M1XLOFEzOTlyM{Gz
MIP human colon carcinoma cell NFXnNnFHfW6ldHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKE2LUDDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDsbY5mNCCLQ{WwQVAvOTJizszN M3j3SFEzOTlyM{Gz
K562 human leukemia cell MVfQdo9tcW[ncnH0bY9vKGG|c3H5 MkfZTY5pcWKrdHnvckBw\iCNNU[yJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1yLkGzJO69VQ>? MVexNlE6ODNzMx?=
MCF-7 tumor cell NV62[oJJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIj6V3hKdmirYnn0bY9vKG:oIF3DSk04KHS3bX;yJINmdGxicILvcIln\XKjdHnvci=> MV[xNFg1OzJzMR?=
human NCI60 cells Mn:3VJJwdGmoZYLheIlwdiCjc4PhfS=> MlnxO|IhcA>? M{\NOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZZN{\XO|ZXSgZZMhdGW2aHHsJIVn\mWldDDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhVEN3ME2wMlkxPCEQvF2= NE[0bY0zOTB6MEewNy=>
PC3 cell NFP0d|FHfW6ldHnvckBie3OjeR?= M2PGOWlvcGmkaYTpc44hd2ZiUFOzJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0yOCEQvF2= MlTuNVExPjN4MEm=
HCT116 cell M3LRR2Z2dmO2aX;uJIF{e2G7 Ml72TY5pcWKrdHnvckBw\iCKQ2SxNVYh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTF|IN88US=> NYLicXlXOTFyNkO2NFk>
A2780 cell MknXSpVv[3Srb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKEF{N{iwJINmdGxiY3zvco9o\W6rYzDhd5Nige,:jDDJR|UxRTF3IN88US=> MoHRNVExPjN4MEm=
Mia PaCa-2 cell NHWyOVdHfW6ldHnvckBie3OjeR?= NHzDPZlKdmirYnn0bY9vKG:oIF3pZUBR[UOjLUKgZ4VtdCClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVM3KM7:TR?= MVyxNVA3OzZyOR?=
human A2780 cells NHXGNWxHfW6ldHnvckBie3OjeR?= M3jVNmlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJG5RVSCyaH;zdIhwenmuYYTpc44h[XRidHjyNVk6KGmwIHj1cYFvKEF{N{iwJINmdGy| MUKxPFQ3QThyOR?=
human A2780 cells MWjGeY5kfGmxbjDhd5NigQ>? MUmyOEBp NU\yS3VoUW6qaXLpeIlwdiCxZjDj[IsudWWmaXH0[YQhWmJicHjvd5Bpd3K7bHH0bY9vKGG2IITodlgzOSCrbjDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB{NDDodpM> M3z2V|E5PDZ7OEC5

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アッセイ
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-eIF4ES209 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-BP1Thr70) 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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

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.
細胞試験:

[5]

- 合併
  • 細胞株: MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562 cells and et al.
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 72 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[5]

- 合併
  • 動物モデル: 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
  • 投薬量: ~7.5 mg/kg/day
  • 投与方法: Injection i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 15 mg/mL (37.32 mM)
Ethanol 8 mg/mL (19.9 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
2.5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 401.84
化学式

C21H20ClNO5

CAS No. 146426-40-6
Storage powder
in solvent
別名 NSC 649890 HCl,HMR-1275
Smiles CN1CCC(C(O)C1)C2=C3OC(=CC(=O)C3=C(O)C=C2O)C4=C(Cl)C=CC=C4

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03441555 Recruiting Drug: Venetoclax|Drug: Alvocidib Acute Myeloid Leukemia (AML) AbbVie|Tolero Pharmaceuticals Inc. May 30 2018 Phase 1
NCT03298984 Completed Drug: Alvocidib|Drug: Cytarabine|Drug: Daunorubicin Acute Myeloid Leukemia Tolero Pharmaceuticals Inc. September 25 2017 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

CDKシグナル伝達経路

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