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Flavopiridol

Cat. No. M1710
Flavopiridol Structure
Synonym:

HMR-1275; Alvocidib; L86-8275

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 50  USD50 In stock
10mg USD 72  USD72 In stock
50mg USD 276  USD276 In stock
100mg USD 396  USD396 In stock
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Quality Control & Documentation
Biological Activity

Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively.

Product Citations
Customer Product Validations & Biological Datas
Source Front Cell Neurosci. 2021 Oct. Figure 4. flavopiridol (Abmole Bioscience, USA)
Method mice treatment
Cell Lines Lgr5+ cells
Concentrations 10 μM
Incubation Time 5 days
Results The flavopiridol treatment decreased both the number (Figure 4c) and diameter of the spheres (Figure 4d), which suggested that inhibition of the SEC could decrease the sphere-forming ability and proliferation ability of Lgr5+ progenitors in vitro.
Protocol (for reference only)
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.
Chemical Information
Molecular Weight 401.84
Formula C21H20ClNO5
CAS Number 146426-40-6
Solubility (25°C) DMSO 15 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Mahoney et al. Blood. ER stress and autophagy: new discoveries in the mechanism of action and drug resistance of the cyclin-dependent kinase inhibitor flavopiridol.

[2] Karp et al. Haematologica. 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.

[3] Kim KS, et al. J Med Chem. Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Flavopiridol, HMR-1275; Alvocidib; L86-8275 supplier, CDK, inhibitors, activators


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