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Flavopiridol hydrochloride is a potent cyclin-dependent kinases inhibitor with an IC50 of 100 nM. Flavopiridol is the first cyclin-dependent kinase inhibitor. At the nanomolar concentrations, flavoporidol hydrochloride prevented rhabdoid cell growth with an IC50 ranging from 50 to 200 nM. Meanwhile, flavopiridol hydrochloride induced G1 and G2 arrest and apoptosis in vitro in a concentration-dependent manner. These influences were associated with the down- regulation of cyclin D1, up- modulation of p21, and induction of caspase 3/7 activities. At a dose of 7.5 mg/kg, flavopiridol markedly suppress the growth of xenografted rhabdoid tumors. That was associated with the induction of p21 and downregulation of cyclin D1. Treatment of flavopiridol decreased the activities of CDK2 and potently prevented cell proliferation with an IC50 ranging from 43 to 83 nM in HNSCC cells.
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Source | Anticancer Res (2017). Figure 4. Flavopiridol hydrochloride |
| Method | Quantification of apoptosis | |
| Cell Lines | CLBl-1 cell line | |
| Concentrations | 100 nM | |
| Incubation Time | 24 h | |
| Results | Preincubation of CLBL-1 cells with the blocking anti-human TRAIL monoclonal antibody (clone RIK2) suppressed the synergistic effect observed when both drugs were used in combination reducing caspase-3/7 activation at same level as that observed with FVP alone. |
 |
Source | Anticancer Res (2017). Figure 2. Flavopiridol hydrochloride |
| Method | Cell death analysis | |
| Cell Lines | CLBL-1 cell line | |
| Concentrations | 250 ng/ml, 500 ng/ml, 1000 ng/ml | |
| Incubation Time | 6 h | |
| Results | FVP alone showed remarkable cytotoxicity on CLBL-1 cells. However, combination of hTRAIL with FVP showed a higher cytotoxic effect that FVP alone. |
| Cell Experiment | |
|---|---|
| Cell lines | SUDHL4, SUDHL6, Jurkat, MOLT4, and HL60 |
| Preparation method | Growing cells at a density of 1 × 106 cells/mL are exposed to Flavopiridol for different concentrations and time periods. DNA is extracted. Briefly, washing cells once with cold phosphate-buffered saline (PBS) and lysing 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. Then digested RNA 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. |
| Concentrations | 0, 100 500, 5000 nM |
| Incubation time | 14 hours |
| Animal Experiment | |
|---|---|
| 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] |
| Molecular Weight | 438.3 |
| Formula | C21H20ClNO5.HCl |
| CAS Number | 131740-09-5 |
| Solubility (25°C) | Water 20 mg/mL DMSO 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] A Tomillero, et al. Gateways to clinical trials
[2] Michael Hallek. State-of-the-art treatment of chronic lymphocytic leukemia
[3] A Tomillero, et al. Gateways to clinical trials
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