Flavopiridol (Alvocidib)

製品コードS1230 別名:NSC 649890 HCl,HMR-1275

Flavopiridol (Alvocidib)化学構造


Flavopiridol (Alvocidib)はATPと一緒に、CDKs(CDK1、CDK2、CDK4とCDK6を含める)を競争性的に抑制して、このIC50値が約40nMになりますが、CDK1、2、4と6に作用する選択性はCDK7に作用する選択性より7.5倍が高くなって、最初に発見したことは EGFRとPKAを抑制することができるということです。臨床 1/2。

サイズ 価格(税別)  
JPY 8300.00
JPY 28220.00
JPY 94620.00


  • (C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50 μM) 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 (Alvocidib) purchased from Selleck.

    G, human THP-1 cells were treated with various small-molecule inhibitors or chemotherapy at increasing concentrations for 24 hours and then analyzed for viability by flow cytometry for PI exclusion. Cells concurrently treated with palbociclib or dinaciclib were analyzed for cytostatis according to nuclear DNA content.

    Cancer Res, 2016, 76(5):1158-69. Flavopiridol (Alvocidib) purchased from Selleck.

  • Pharmacological inhibition of either CDK1/2 or E2F1 prevented the induction of the expression of MAD2 by SKP2 overexpression. Notes: (A) Human lung cancer A549 cells were transfected with 2 μg of vector pcDNA3.1 or pcDNA-SKP2 for 48 h, then treated with CDK1/2 inhibitor flavopiridol or E2F1 inhibitor HLM006474 for additional 24 h. Total RNAs were extracted for the detection of the mRNA levels MAD2 by RT-QPCR with GAPDH as internal control. Quantitative analysis are expressed as mean ± SEM. n=3, *P<0.05 vs control. (B) Human lung cancer A549 cells were transfected with 2 μg of vector pcDNA3.1 or pcDNA-SKP2 for 48 h, then treated with CDK1/2 inhibitor flavopiridol or E2F1 inhibitor HLM006474 for additional 24 h. Total proteins were extracted for the detection of the protein levels Skp2 and Mad2 and the phosphorylation of Rb at Ser780 (pRb-S780) by Western blotting. GAPDH served as the loading control. (C) Human lung cancer A549 cells were transfected with 50 nM control or SKP2-specific siRNA with lipofectamine 2000 for 48 h, then treated with CDK1/2 inhibitor flavopiridol or E2F1 inhibitor HLM006474 for additional 24 h. Total proteins were extracted for the detection of the protein levels Skp2 and Mad2 by Western blotting. GAPDH served as the loading control. Abbreviations: MAD2, mitotic arrest deficient 2; SKP2, S-phase kinase-associated protein 2; mRNA, messenger RNA; SEM, standard error of the mean; Rb, retinoblastoma; siRNA, small interfering RNA.

    Onco Targets Ther, 2017, 10:439-446. Flavopiridol (Alvocidib) purchased from Selleck.




製品説明 Flavopiridol (Alvocidib)はATPと一緒に、CDKs(CDK1、CDK2、CDK4とCDK6を含める)を競争性的に抑制して、このIC50値が約40nMになりますが、CDK1、2、4と6に作用する選択性はCDK7に作用する選択性より7.5倍が高くなって、最初に発見したことは EGFRとPKAを抑制することができるということです。臨床 1/2。
特性 First CDK inhibitor to be used in human clinical trials.
CDK1 [1] CDK2 [1] CDK4 [1] CDK6 [1] CDK7 [1]
40 nM 40 nM 40 nM 40 nM 300 nM

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ID8 cells NVm0bWFxWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn2xRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDJSFgh[2WubIOsJGlEPTB;NzDuUS=> NGe4S|cyPzF{M{iyNS=>
Sf9 cells M4S2dmZ2dmO2aX;uJIF{e2G7 NH;iWVJKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIN6[2yrbjDBM2NFUzJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2xNkBvVQ>? NUnQfnMzOTd7MESzOlY>
LNCaP human prostate carcinoma cell MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M3e2PWlvcGmkaYTpc44hd2ZiTF7DZXAhcHWvYX6gdJJwe3SjdHWgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvci=> NGnQXXAyOjF7MEOxNy=>
HCT116/VP35 human colon carcinoma cell M2[2fXBzd2yrZnXyZZRqd25iYYPzZZk> NFS1fWZKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= NGrRcIUyOjF7MEOxNy=>
HCT116 human colon carcinoma cell NWX3TYVHWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2PE[2lvcGmkaYTpc44hd2ZiSFPUNVE3KGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MUigcm0> MlnFNVIyQTB|MUO=
HCT116/VM46 human colon carcinoma cell M{j2fnBzd2yrZnXyZZRqd25iYYPzZZk> M1Pzd2lvcGmkaYTpc44hd2ZiSFPUNVE3N1[PNE[gbJVu[W5iY3;sc44h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0zOSCwTR?= NHTne2kyOjF7MEOxNy=>
human A2780 cells M1jEXmN6fG:2b4jpZ:Kh[XO|YYm= M4nnVFI1KGh? MmL6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yN{BvVQ>? NFTCenQzOzNyMUe2Oy=>
MCF7 cells Mom0VJJwdGmoZYLheIlwdiCjc4PhfS=> MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOsJGlEPTB;Mk[gcm0> NGC1[VEyPzF{M{iyNS=>
human MRC5 cells NIrOUoZEgXSxdH;4bYPDqGG|c3H5 MnTIO|IhcA>? Mor3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUK4JI5O MUWyN|MxOTd4Nx?=
human A2780 cells MnfpR5l1d3SxeHnjxsBie3OjeR?= MnnrO|IhcA>? NYHBdnJXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0zQSCwTR?= NILiPJIzOzNyMUe2Oy=>
human A2780 cells NF;hOpZEgXSxdH;4bYPDqGG|c3H5 M4jGR|Q5KGh? NXXmd21[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0{OSCwTR?= MlLjNlM{ODF5Nke=
A2780/DDP-R human ovarian carcinoma cell M1rpT3Bzd2yrZnXyZZRqd25iYYPzZZk> MoTZTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUjDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:Ozhibl2= M{TUOVEzOTlyM{Gz
human MRC5 cells NWjRRndRS3m2b4TvfIlkyqCjc4PhfS=> M4PDSFQ5KGh? MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> NX\YRWFZOjN|MEG3Olc>
ABAE human fibroblast cell NHK3U2VRem:uaX\ldoF1cW:wIHHzd4F6 MX7Jcohq[mm2aX;uJI9nKEGEQVWgbJVu[W5iZnnido9jdGG|dDDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NEWgcm0> MVixNlE6ODNzMx?=
HL60 human leukemia cell NHTnOWRRem:uaX\ldoF1cW:wIHHzd4F6 NIrvVpFKdmirYnn0bY9vKG:oIFjMOlAhcHWvYX6gcIV2c2WvaXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPUS2JI5O MUWxNlE6ODNzMx?=
human MRC5 cells NXLifmFGS3m2b4TvfIlkyqCjc4PhfS=> MX2yOEBp NYrSS4IxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVQ6KG6P NFTZc4IzOzNyMUe2Oy=>
Hs 27 human fibroblast cell NXLjUW41WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUTCcYFMUW6qaXLpeIlwdiCxZjDId{AzPyCqdX3hckBncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OSCwTR?= NXvUWlR5OTJzOUCzNVM>
CCRF-CEM human leukemia cell NFuySGdRem:uaX\ldoF1cW:wIHHzd4F6 NGjDbmtKdmirYnn0bY9vKG:oIFPDVmYuS0WPIHj1cYFvKGyndXvlcYliKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF02OiCwTR?= NWLsWIdDOTJzOUCzNVM>
OVCAR-3 human ovarian carcinoma cell MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MmP5TY5pcWKrdHnvckBw\iCRVlPBVk0{KGi3bXHuJI93[XKrYX6gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME21OEBvVQ>? MXuxNlE6ODNzMx?=
A2780/DDP-S human ovarian carcinoma cell MmDaVJJwdGmoZYLheIlwdiCjc4PhfS=> NFPmfIJKdmirYnn0bY9vKG:oIFGyO|gxN0SGUD3TJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD13NjDuUS=> NFXsSJAyOjF7MEOxNy=>
human HMEC1 cells M4KxW2N6fG:2b4jpZ:Kh[XO|YYm= NFHYe2szPCCq NWn6eo0zS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE2HQ{GgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF03OSCwTR?= MU[yN|MxOTd4Nx?=
human HMEC1 cells MnHBR5l1d3SxeHnjxsBie3OjeR?= MmLsOFghcA>? NV3Dc|NbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE2HQ{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF03OiCwTR?= MkTRNlM{ODF5Nke=
A2780/TAX-S human ovarian carcinoma cell MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NVXSWJV5UW6qaXLpeIlwdiCxZjDBNlc5OC:WQWitV{BpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;NkWgcm0> MmnDNVIyQTB|MUO=
LS174T human colon carcinoma cell NGT3XmhRem:uaX\ldoF1cW:wIHHzd4F6 NHjFVIdKdmirYnn0bY9vKG:oIFzTNVc1XCCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[1JI5O M2rj[lEzOTlyM{Gz
MCF-7 human breast carcinoma cell M1TJPHBzd2yrZnXyZZRqd25iYYPzZZk> NIrKZm1KdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O M3TV[VEzOTlyM{Gz
human HMEC1 cells NFLGZ5lEgXSxdH;4bYPDqGG|c3H5 MVW3NkBp Ml7PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTG1GSzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME22OkBvVQ>? MUOyN|MxOTd4Nx?=
PC3 human prostate carcinoma cell NFHVeW9Rem:uaX\ldoF1cW:wIHHzd4F6 MYrJcohq[mm2aX;uJI9nKFCFMzDoeY1idiCycn;zeIF1\SClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTZ4IH7N MUexNlE6ODNzMx?=
human A2780 cell line Ml;UVJJwdGmoZYLheIlwdiCjc4PhfS=> MXO3NkBp Mn\LRY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9O|Ehdk1? M1rObVE2ODJ5OE[z
human ovarian (A2780) cancer cell MUjDfZRwfG:6aXRCpIF{e2G7 MVvDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P MYixOVEzPTl5MR?=
MLF mouse lung fibroblast cell MkLzVJJwdGmoZYLheIlwdiCjc4PhfS=> MkXoTY5pcWKrdHnvckBw\iCPTF[gcY92e2VibIXu[{BncWK{b3LsZZN1KGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF04OiCwTR?= MlrRNVIyQTB|MUO=
human NCI60 cells NHXUNYVRem:uaX\ldoF1cW:wIHHzd4F6 MmnMO|IhcA>? NGrwTphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTVYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCJSUWwQVc1Njdibl2= M3zHOVIyODhyN{Cz
LX-1 human lung carcinoma Mn6yVJJwdGmoZYLheIlwdiCjc4PhfS=> NInKSlVKdmirYnn0bY9vKG:oIFzYMVEhcHWvYX6gcJVv\yClYYLjbY5wdWFicILvcIln\XKjdHnvckwhUUN3ME23OUBvVQ>? M2XySFEzOTlyM{Gz
A431 human squamous cell NX\WVIN3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEfLdYpKdmirYnn0bY9vKG:oIFG0N|EhcHWvYX6gd5F2[W2xdYOgZ4VtdCClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTd3IH7N MYixNlE6ODNzMx?=
SKBR-3 human breast carcinoma cell MnzNVJJwdGmoZYLheIlwdiCjc4PhfS=> NWXQ[WpDUW6qaXLpeIlwdiCxZjDTT2JTNTNiaIXtZY4h[nKnYYP0JINiemOrbn;tZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9O|chdk1? MmjTNVIyQTB|MUO=
A2780/TAX-R human ovarian carcinoma cell NXLuRYFpWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUTIWnRVUW6qaXLpeIlwdiCxZjDBNlc5OC:WQWitVkBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;N{igcm0> MYSxNlE6ODNzMx?=
M109 mouse lung carcinoma cell MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NF;n[|BKdmirYnn0bY9vKG:oIF2xNFkhdW:3c3WgcJVv\yClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRThyIH7N NHfrWG4yOjF7MEOxNy=>
CACO-2 human colon carcinoma cell MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MkHUTY5pcWKrdHnvckBw\iCFQVPPMVIhcHWvYX6gZ49td25iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD16NjDuUS=> MoPKNVIyQTB|MUO=
A549 human lung carcinoma cell NGPz[HdRem:uaX\ldoF1cW:wIHHzd4F6 NWrIeWZkUW6qaXLpeIlwdiCxZjDBOVQ6KGi3bXHuJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD17NjDuUS=> NYXxXmRuOTJzOUCzNVM>
MIP human colon carcinoma cell NVuwNHBnTnWwY4Tpc44h[XO|YYm= NIDtTohKdmirYnn0bY9vKG:oIF3JVEBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBtcW6nLDDJR|UxRTBwMUKg{txO MWexNlE6ODNzMx?=
K562 human leukemia cell M3nSXXBzd2yrZnXyZZRqd25iYYPzZZk> NUL3XopxUW6qaXLpeIlwdiCxZjDLOVYzKGi3bXHuJIxmfWunbXnhJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlE{KM7:TR?= NE\Y[mQyOjF7MEOxNy=>
MCF-7 tumor cell NInIb2dRem:uaX\ldoF1cW:wIHHzd4F6 M3nqTGlvcGmkaYTpc44hd2ZiTVPGMVchfHWvb4KgZ4VtdCCycn;sbYZmemG2aX;u MWqxNFg1OzJzMR?=
human NCI60 cells NHXUXYVRem:uaX\ldoF1cW:wIHHzd4F6 NVrvT3dlPzJiaB?= NXvSR2p[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bie3Onc4Pl[EBieyCuZYToZYwh\W[oZXP0JIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCOQ{WwQVAvQTB2IN88US=> MUSyNVA5ODdyMx?=
PC3 cell NV3OT4NoTnWwY4Tpc44h[XO|YYm= NUnreoxmUW6qaXLpeIlwdiCxZjDQR|Mh[2WubDDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTFyIN88US=> MWWxNVA3OzZyOR?=
HCT116 cell NGnSdWtHfW6ldHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKEiFVEGxOkBk\WyuIHPsc45w\2WwaXOgZZN{[XluIFnDOVA:OTNizszN MonvNVExPjN4MEm=
A2780 cell NWXkVXI{TnWwY4Tpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKEF{N{iwJINmdGxiY3zvco9o\W6rYzDhd5Nige,:jDDJR|UxRTF3IN88US=> MnjGNVExPjN4MEm=
Mia PaCa-2 cell M4HHOWZ2dmO2aX;uJIF{e2G7 NXj4XlZGUW6qaXLpeIlwdiCxZjDNbYEhWGGFYT2yJINmdGxiY3zvco9o\W6rYzDhd5NigSxiSVO1NF0{PiEQvF2= MXuxNVA3OzZyOR?=
human A2780 cells M2D2WmZ2dmO2aX;uJIF{e2G7 M4LNfGlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJG5RVSCyaH;zdIhwenmuYYTpc44h[XRidHjyNVk6KGmwIHj1cYFvKEF{N{iwJINmdGy| MmfLNVg1Pjl6MEm=
human A2780 cells NGj1eJNHfW6ldHnvckBie3OjeR?= NEX0coQzPCCq M1rsS2lvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCC2aIK4NlEhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILz MUSxPFQ3QThyOR?=


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]




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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.


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  • 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.



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  • 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
  • 製剤: Dissolved in a mixture of Cremophor/ethanol (50:50), and diluted in water
  • 投薬量: ~7.5 mg/kg/day
  • 投与方法: Injection i.p.

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 順序で溶剤を入れること:
5% DMSO+30% PEG 300+ddH2O

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 401.84


CAS No. 146426-40-6
別名 NSC 649890 HCl,HMR-1275





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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


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

  • C1



  • 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):




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


マス 濃度 ボリューム 分子量


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
NCT02520011 Recruiting Acute Myeloid Leukemia Tolero Pharmaceuticals, Inc. December 2015 Phase 2
NCT01349972 Completed Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome|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 Del(5q)|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)|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) April 2011 Phase 2
NCT01076556 Terminated Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage I Small Lymphocytic Lymphoma|Stage II Chronic Lymphocytic Leukemia|Stage II Small Lymphocytic Lymphoma|Stage III Chronic Lymphocytic Leukemia|Stage III Small Lymphocytic Lymphoma|Stage IV Chronic Lymphocytic Leukemia|Stage IV Small Lymphocytic Lymphoma National Cancer Institute (NCI) April 2010 Phase 1
NCT00991952 Completed Adenocarcinoma of the Gastroesophageal Junction|Diffuse Adenocarcinoma of the Stomach|Intestinal Adenocarcinoma of the Stomach|Mixed Adenocarcinoma of the Stomach|Recurrent Gastric Cancer|Stage IIIA Gastric Cancer|Stage IIIB Gastric Cancer|Stage IIIC Gastric Cancer|Stage IV Gastric Cancer National Cancer Institute (NCI) September 2009 Phase 2
NCT00957905 Completed Recurrent Extragonadal Seminoma|Recurrent Malignant Extragonadal Germ Cell Tumor|Recurrent Malignant Extragonadal Non-Seminomatous Germ Cell Tumor|Recurrent Malignant Testicular Germ Cell Tumor|Recurrent Ovarian Germ Cell Tumor|Stage III Testicular Cancer|Stage IV Extragonadal Non-Seminomatous Germ Cell Tumor|Stage IV Extragonadal Seminoma|Stage IV Ovarian Germ Cell Tumor National Cancer Institute (NCI) June 2009 Phase 2



Handling Instructions


  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID