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Flavopiridol hydrochloride

Cat. No. M3483
Flavopiridol hydrochloride Structure
Synonym:

NSC 649890 HCl

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 280 In stock
100mg USD 440 In stock
200mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Flavopiridol hydrochloride is a potent cyclin-dependent kinases inhibitor with an IC50 of 100 nM. Preclinically, 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.

Protocol
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]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 438.3
Formula C21H20ClNO5.HCl
CAS Number 131740-09-5
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
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.
Rating
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.
Rating
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Flavopiridol hydrochloride, NSC 649890 HCl supplier, CDK, inhibitors

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