Flavopiridol hydrochloride

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Cat.No. 3094 - Flavopiridol hydrochloride | C21H20ClNO5.HCl | CAS No. 131740-09-5
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)
Datasheet
Citations (1)
Reviews
Literature (4)

Biological Activity

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

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

Technical Data

M. Wt 438.3
Formula C21H20ClNO5.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 131740-09-5
PubChem ID 9910986
InChI Key LGMSNQNWOCSPIK-LWHGMNCYSA-N
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

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

Preparing Stock Solutions

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

Molarity Calculator

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References

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


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Keywords: Flavopiridol hydrochloride, Flavopiridol hydrochloride supplier, L86-8275, HMR1275, cyclin, dependent, kinases, inhibitors, inhibits, CDKs, cell, cycle, arrest, antitumor, antiproliferative, anticancer, L, 86-8275, Cyclin-dependent, Kinase, 3094, Tocris Bioscience

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


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Literature in this Area

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