Flavopiridol HCl

For research use only.

Catalog No.S2679 Synonyms: NSC 649890 HCl, alvocidib, L86-8275, HMR-1275, DSP-2033

21 publications

Flavopiridol HCl Chemical Structure

CAS No. 131740-09-5

Flavopiridol HCl (NSC 649890 HCl, alvocidib, L86-8275, HMR-1275, DSP-2033) 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. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.

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Selleck's Flavopiridol HCl has been cited by 21 publications

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Choose Selective CDK Inhibitors

Biological Activity

Description Flavopiridol HCl (NSC 649890 HCl, alvocidib, L86-8275, HMR-1275, DSP-2033) 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. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. 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 MWnQdo9tcW[ncnH0bY9vKGG|c3H5 M1zrSmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTWQ5KGOnbHzzMEBKSzVyPUegcm0> MXOxO|EzOzh{MR?=
Sf9 cells Mk\vSpVv[3Srb36gZZN{[Xl? NFnEeZZKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIN6[2yrbjDBM2NFUzJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2xNkBvVQ>? M2PQcFE4QTB2M{[2
LNCaP human prostate carcinoma cell NWX4WGRNWHKxbHnm[ZJifGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKEyQQ3HQJIh2dWGwIIDyc5N1[XSnIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36= MnXwNVIyQTB|MUO=
HCT116/VP35 human colon carcinoma cell NEn4doJRem:uaX\ldoF1cW:wIHHzd4F6 NG\6c4RKdmirYnn0bY9vKG:oIFjDWFEyPi:YUEO1JIh2dWGwIHPvcI9vKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OTdibl2= NEH5dmcyOjF7MEOxNy=>
HCT116 human colon carcinoma cell NFHC[XdRem:uaX\ldoF1cW:wIHHzd4F6 NVzDbZpUUW6qaXLpeIlwdiCxZjDIR3QyOTZiaIXtZY4h[2:ub36gZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2xPEBvVQ>? NETUcJUyOjF7MEOxNy=>
HCT116/VM46 human colon carcinoma cell MoXXVJJwdGmoZYLheIlwdiCjc4PhfS=> NYLBSHlqUW6qaXLpeIlwdiCxZjDIR3QyOTZxVl20OkBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTJzIH7N M2PNPFEzOTlyM{Gz
human A2780 cells MYTDfZRwfG:6aXRCpIF{e2G7 Mo\tNlQhcA>? MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUKzJI5O NGPYbYMzOzNyMUe2Oy=>
MCF7 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOsJGlEPTB;Mk[gcm0> NED3cJkyPzF{M{iyNS=>
human MRC5 cells NH3WNmREgXSxdH;4bYPDqGG|c3H5 MVW3NkBp NGHBc4FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9Nlghdk1? NVHpUXpVOjN|MEG3Olc>
human A2780 cells Mmm2R5l1d3SxeHnjxsBie3OjeR?= NVjG[4VRPzJiaB?= Mo\iR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2yPUBvVQ>? M4K2eVI{OzBzN{[3
human A2780 cells M1XRZmN6fG:2b4jpZ:Kh[XO|YYm= NX\QZW9RPDhiaB?= NX:3VGVvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF0{OSCwTR?= NI\4W4MzOzNyMUe2Oy=>
A2780/DDP-R human ovarian carcinoma cell MWjQdo9tcW[ncnH0bY9vKGG|c3H5 MYXJcohq[mm2aX;uJI9nKEF{N{iwM2RFWC2UIHj1cYFvKG:4YYLpZY4h[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF0{QCCwTR?= Mme0NVIyQTB|MUO=
human MRC5 cells Mo\uR5l1d3SxeHnjxsBie3OjeR?= MXu0PEBp MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;M{mgcm0> M4nQfVI{OzBzN{[3
ABAE human fibroblast cell NH3tUFVRem:uaX\ldoF1cW:wIHHzd4F6 NUDCcFdyUW6qaXLpeIlwdiCxZjDBRmFGKGi3bXHuJIZq[nKxYnzhd5Qh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVQ2KG6P M{m0fFEzOTlyM{Gz
HL60 human leukemia cell MYXQdo9tcW[ncnH0bY9vKGG|c3H5 Mk\nTY5pcWKrdHnvckBw\iCKTE[wJIh2dWGwIHzleYtmdWmjIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD12NjDuUS=> MmrlNVIyQTB|MUO=
human MRC5 cells M{LJZmN6fG:2b4jpZ:Kh[XO|YYm= NWGzVIw2OjRiaB?= M1H4PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME20PUBvVQ>? MofCNlM{ODF5Nke=
Hs 27 human fibroblast cell MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 M{TqeGlvcGmkaYTpc44hd2ZiSIOgNlchcHWvYX6g[oljem:kbHHzeEBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVEhdk1? MVuxNlE6ODNzMx?=
CCRF-CEM human leukemia cell NYryOpdQWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmG1TY5pcWKrdHnvckBw\iCFQ2LGMWNGVSCqdX3hckBt\XWtZX3pZUBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9OVIhdk1? NFjXUWcyOjF7MEOxNy=>
OVCAR-3 human ovarian carcinoma cell NYe0W25nWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGnleVZKdmirYnn0bY9vKG:oIF;WR2FTNTNiaIXtZY4hd3[jcnnhckBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVU1KG6P NE\vNnIyOjF7MEOxNy=>
A2780/DDP-S human ovarian carcinoma cell NHfSeW5Rem:uaX\ldoF1cW:wIHHzd4F6 MmDyTY5pcWKrdHnvckBw\iCDMke4NE9FTFBvUzDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PTZibl2= MWSxNlE6ODNzMx?=
human HMEC1 cells NXHS[5dsS3m2b4TvfIlkyqCjc4PhfS=> MkCwNlQhcA>? M{jKOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhOTUNzIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEeLNUC9OlEhdk1? MlXVNlM{ODF5Nke=
human HMEC1 cells NU\0RplTS3m2b4TvfIlkyqCjc4PhfS=> Mkn4OFghcA>? MoXqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTG1GSzFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME22NkBvVQ>? M1jBN|I{OzBzN{[3
A2780/TAX-S human ovarian carcinoma cell Mly3VJJwdGmoZYLheIlwdiCjc4PhfS=> NHfOWW9KdmirYnn0bY9vKG:oIFGyO|gxN1SDWD3TJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD14NTDuUS=> NXrzR49JOTJzOUCzNVM>
LS174T human colon carcinoma cell MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NIS0cWlKdmirYnn0bY9vKG:oIFzTNVc1XCCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[1JI5O Mo\wNVIyQTB|MUO=
MCF-7 human breast carcinoma cell NWHlUFlbWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGPIN2JKdmirYnn0bY9vKG:oIF3DSk04KGi3bXHuJIJz\WG|dDDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O NGjQW3UyOjF7MEOxNy=>
human HMEC1 cells Ml3lR5l1d3SxeHnjxsBie3OjeR?= MWm3NkBp MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBIUTVyPU[2JI5O NVPOVZV3OjN|MEG3Olc>
PC3 human prostate carcinoma cell NH\zbFNRem:uaX\ldoF1cW:wIHHzd4F6 NHe3U|FKdmirYnn0bY9vKG:oIGDDN{BpfW2jbjDwdo9{fGG2ZTDjZZJkcW6xbXGgZ4VtdCCycn;sbYZmemG2aX;uMEBKSzVyPU[2JI5O MVuxNlE6ODNzMx?=
human A2780 cell line NYjaO4FiWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV:3NkBp NUH3N3BySW62aYDyc4xq\mW{YYTpeoUh\W[oZXP0JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubDDsbY5mKHejczDk[ZRmem2rbnXkJIlvKGFid3jvcIUh[2WubDC3NkBpeiCleYTveI95cWOrdImgZZN{[XluIFnDOVA:PzFibl2= MkHxNVUxOjd6NkO=
human ovarian (A2780) cancer cell MoS5R5l1d3SxeHnjxsBie3OjeR?= MYfDfZRwfG:6aXOg[YZn\WO2IH;uJIh2dWGwIH;2ZZJq[W5iKFGyO|gxMSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVcyKG6P NUK4eI1nOTVzMkW5O|E>
MLF mouse lung fibroblast cell M1zvbXBzd2yrZnXyZZRqd25iYYPzZZk> M3PWRmlvcGmkaYTpc44hd2ZiTVzGJI1wfXOnIHz1coch\mmkcn;icIF{fCClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:PzJibl2= M3PuNVEzOTlyM{Gz
human NCI60 cells NIDkXXdRem:uaX\ldoF1cW:wIHHzd4F6 MnPvO|IhcA>? NX;I[4gzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF04PC55IH7N MV2yNVA5ODdyMx?=
LX-1 human lung carcinoma NYnaO5JMWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3zXZ2lvcGmkaYTpc44hd2ZiTGitNUBpfW2jbjDseY5oKGOjcnPpco9u[SCycn;sbYZmemG2aX;uMEBKSzVyPUe1JI5O M2LXeFEzOTlyM{Gz
A431 human squamous cell M4jqdXBzd2yrZnXyZZRqd25iYYPzZZk> MVzJcohq[mm2aX;uJI9nKEF2M{GgbJVu[W5ic4H1ZY1wfXNiY3XscEBk[XKlaX7vcYEh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVc2KG6P M4LQblEzOTlyM{Gz
SKBR-3 human breast carcinoma cell NFK4T4FRem:uaX\ldoF1cW:wIHHzd4F6 NFm5OplKdmirYnn0bY9vKG:oIGPLRnIuOyCqdX3hckBjemWjc4SgZ4Fz[2mwb33hJINmdGxicILvcIln\XKjdHnvckwhUUN3ME23O{BvVQ>? M3\wPFEzOTlyM{Gz
A2780/TAX-R human ovarian carcinoma cell MXzQdo9tcW[ncnH0bY9vKGG|c3H5 NID6TW5KdmirYnn0bY9vKG:oIFGyO|gxN1SDWD3SJIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD15ODDuUS=> NVvXTpJbOTJzOUCzNVM>
M109 mouse lung carcinoma cell MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 MontTY5pcWKrdHnvckBw\iCPMUC5JI1wfXOnIHz1coch[2G{Y3nuc41iKGOnbHygdJJwdGmoZYLheIlwdixiSVO1NF05OCCwTR?= M{DRSVEzOTlyM{Gz
CACO-2 human colon carcinoma cell NVjjdowzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3TZOmlvcGmkaYTpc44hd2ZiQ1HDU{0zKGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;OE[gcm0> M2S5OVEzOTlyM{Gz
A549 human lung carcinoma cell MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NYKzXJJoUW6qaXLpeIlwdiCxZjDBOVQ6KGi3bXHuJIx2dmdiY3HyZ4lvd22jIHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD17NjDuUS=> NXXrNVd[OTJzOUCzNVM>
MIP human colon carcinoma cell MnPvSpVv[3Srb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKE2LUDDoeY1idiClb3zvckBk[XKlaX7vcYEh[2WubDDsbY5mNCCLQ{WwQVAvOTJizszN MXSxNlE6ODNzMx?=
K562 human leukemia cell MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 MXHJcohq[mm2aX;uJI9nKEt3NkKgbJVu[W5ibHX1b4VucWFiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTBwMUOg{txO NViy[HRoOTJzOUCzNVM>
MCF-7 tumor cell MmrZVJJwdGmoZYLheIlwdiCjc4PhfS=> NXrVeGM3UW6qaXLpeIlwdiCxZjDNR2YuPyC2dX3vdkBk\WyuIIDyc4xq\mW{YYTpc44> MkPZNVA5PDN{MUG=
human NCI60 cells MojsVJJwdGmoZYLheIlwdiCjc4PhfS=> MYi3NkBp M3zuT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOgZZN{\XO|ZXSgZZMhdGW2aHHsJIVn\mWldDDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhVEN3ME2wMlkxPCEQvF2= MUCyNVA5ODdyMx?=
PC3 cell NHvHWndHfW6ldHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKFCFMzDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9NVAh|ryP MmPRNVExPjN4MEm=
HCT116 cell MoLhSpVv[3Srb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKEiFVEGxOkBk\WyuIHPsc45w\2WwaXOgZZN{[XluIFnDOVA:OTNizszN NV;Jb|gyOTFyNkO2NFk>
A2780 cell NFfJOmZHfW6ldHnvckBie3OjeR?= NIexZpFKdmirYnn0bY9vKG:oIFGyO|gxKGOnbHygZ4xwdm:pZX7pZ{Bie3Ojef-8kEBKSzVyPUG1JO69VQ>? M2T3TVEyODZ|NkC5
Mia PaCa-2 cell M{fYfWZ2dmO2aX;uJIF{e2G7 M{fWbWlvcGmkaYTpc44hd2ZiTXnhJHBiS2FvMjDj[YxtKGOub37v[4VvcWNiYYPzZZktKEmFNUC9N|Yh|ryP M1rRblEyODZ|NkC5
human A2780 cells MVPGeY5kfGmxbjDhd5NigQ>? NGrZXYdKdmirYnn0bY9vKG:oIHPkb{1u\WSrYYTl[EBPWE1icHjvd5Bpd3K7bHH0bY9vKGG2IITodlE6QSCrbjDoeY1idiCDMke4NEBk\Wyucx?= Mn3PNVg1Pjl6MEm=
human A2780 cells MYnGeY5kfGmxbjDhd5NigQ>? MkDWNlQhcA>? M2DuOWlvcGmkaYTpc44hd2ZiY3TrMY1m\GmjdHXkJHJjKHCqb4PwbI9zgWyjdHnvckBifCC2aIK4NlEhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOjRiaILz MonwNVg1Pjl6MEm=

... Click to View More Cell Line Experimental Data

Assay
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-eIF4E(S209) 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-BP1(Thr70)] 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
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]
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  • 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
  • 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, alvocidib, L86-8275, HMR-1275, DSP-2033
Smiles CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID