Flavopiridol hydrochloride

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Description: Cdk inhibitor; potently inhibits cdk2 and cdk9
Alternative Names: L 86-8275
Chemical Name: 2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one hydrochloride
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for Flavopiridol hydrochloride

Flavopiridol hydrochloride is a cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 6 - 25 nM and 84 - 200 nM for cdk9 and cdk2, respectively, and <0.85 μM for cdk1, cdk4, cdk5 and cdk7). Induces cell cycle arrest at G1 and G2 phase. Potently inhibits the growth of breast and lung cancer cell lines (IC50 = 25 - 160 nM) in vitro.

Compound Libraries for Flavopiridol hydrochloride

Flavopiridol hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Flavopiridol hydrochloride

M. Wt 438.3
Formula C21H20ClNO5.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 131740-09-5
PubChem ID 9910986
Smiles CN(CC3)C[C@@H](O)[C@H]3[C@]1=C(OC(C4=CC=CC=C4Cl)=CC2=O)C2=C(O)C=C1O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Flavopiridol hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 43.83 100
DMSO 43.83 100

Preparing Stock Solutions for Flavopiridol hydrochloride

The following data is based on the product molecular weight 438.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.41 mL 22.82 mL
5 mM 0.46 mL 2.28 mL 4.56 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets for Flavopiridol hydrochloride

References for Flavopiridol hydrochloride

References are publications that support the biological activity of the product.

Kaur et al (1992) Growth inhibition with reversible cell cycle arrest of carcinoma cells by Flavone L86-8275. J.Natl.Cancer.Inst. 84 1736 PMID: 1279187

Ambrosini et al (2008) The cyclin-dependent kinase inhibitor flavopiridol potentiates the effects of topoisomerase I poisons by suppressing Rad51 expression in a p53-dependent manner. Cancer Res. 68 2312 PMID: 18381438

Losiewicz et al (1994) Potent inhibition of Cdc2 kinase activity by the flavonoid L86-8275. Biochem.Biophys.Res.Comm. 201 589

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

If you know of a relevant reference for Flavopiridol hydrochloride, please let us know.

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1 Citation for Flavopiridol hydrochloride

Citations are publications that use Tocris products. Selected citations for Flavopiridol hydrochloride include:

Stork et al (2016) Co-transcriptional R-loops are the main cause of estrogen-induced DNA damage. Elife 5 PMID: 27552054

Do you know of a great paper that uses Flavopiridol hydrochloride from Tocris? Please let us know.

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