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Flavopiridol

Cat. No. M1710
Flavopiridol Structure
Synonym:

Alvocidib, HMR-1275

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 80 In stock
50mg USD 250 In stock
100mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Flavopiridol (Alvocidib) is a potent inhibitor of CDKs 1, 2 and 4 in cell-free assays (IC50 in the region of 100 nM) and tumour cell growth in vitro (typical IC50 in the region of 100 nM). Flavopiridol is effective in inducing cell cycle arrest and cytotoxicity in rhabdoid tumors. Its effects are correlated with the down-regulation of cyclin D1 and the up-regulation of p21. Flavopiridol is potentially a novel chemotherapeutic agent for rhabdoid tumors.

Protocol
Cell Experiment
Cell lines ovarian tumor cell line A2780/ DDP-S
Preparation method 72 h Proliferation Assay. In vitro cytotoxicity was assessed in tissue culture cells by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfenyl)-2H-tetrazolium, inner salt) assay as previously described.23 Depending upon the cell line used, cells were plated at a density of 3000- 6000 cells/well, in a 96 well plate, and 24 h later, drugs were added and serial-diluted. The cells were incubated at 37 °C for 72 h at which time the tetrazolium dye, MTS in combination with phenazine methosulfate, was added. After 3 h, the absorbency was measured at 492 nm, which is proportional to the number of viable cells. The results are expressed as IC50 values.
Concentrations 0~10 μM
Incubation time 72 h
Animal Experiment
Animal models A2780 human ovarian carcinoma xenograft model in nude mice
Formulation dissolved in a mixture of Cremophor/ ethanol (50:50) , final dilution to the required dosage strength was made with water
Dosages 7.5mg/kg qdx8
Administration i.p.
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 401.84
Formula C21H20ClNO5
CAS Number 146426-40-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

ER stress and autophagy: new discoveries in the mechanism of action and drug resistance of the cyclin-dependent kinase inhibitor flavopiridol.
Mahoney et al. Blood. 2012 Aug 9;120(6):1262-73. PMID: 22740450.

Randomized phase II study of two schedules of flavopiridol given as timed sequential therapy with cytosine arabinoside and mitoxantrone for adults with newly diagnosed, poor-risk acute myelogenous leukemia.
Karp et al. Haematologica. 2012 Jun 24. PMID: 22733022.

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, et al. J Med Chem. 2002 Aug 29;45(18):3905-27. PMID: 12190313.

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Keywords: Flavopiridol, Alvocidib, HMR-1275 supplier, CDK, inhibitors

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