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Description: Potent covalent CDK14 and CDK16 inhibitor; also inhibits other TAIRE kinase family members
Chemical Name: N-[1-[[3-[[(2E)-4-(Dimethylamino)-1-oxo-2-buten-1-yl]amino]phenyl]sulfonyl]-4-piperidinyl]-4-[(2,4,6- trichlorobenzoyl)amino]-1H-pyrazole-3-carboxamide
Purity: ≥98% (HPLC)

Biological Activity for FMF-04-159-2

FMF-04-159-2 is a potent inhibitor of CDK14 and CDK16 (IC50 = 40 nM for CDK14 in cellular BRET assay; IC50 values are 88 and 10 nM for CDK14 and CDK16 in kinase activity inhibition assay, respectively). Inhibits other TAIRE kinase family members at 1 μM (CDK17 and CDK18). Also binds CDK2 (IC50 = 256 nM). Displays covalent binding of CDK14, with binding sustained after washout. Causes cell cycle arrest at G2/M in cancer cell lines.

Reversible control FMF-04-159-R (Cat. No. 7159) also available.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Compound Libraries for FMF-04-159-2

FMF-04-159-2 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 FMF-04-159-2

M. Wt 683.01
Formula C28H30Cl3N7O5S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2364489-81-4
Smiles CN(C/C=C/C(NC1=CC=CC(S(=O)(N2CCC(NC(C3=NNC=C3NC(C4=C(C=C(C=C4Cl)Cl)Cl)=O)=O)CC2)=O)=C1)=O)C

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 FMF-04-159-2

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 68.3 100
ethanol 13.66 20

Preparing Stock Solutions for FMF-04-159-2

The following data is based on the product molecular weight 683.01. 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 1.46 mL 7.32 mL 14.64 mL
5 mM 0.29 mL 1.46 mL 2.93 mL
10 mM 0.15 mL 0.73 mL 1.46 mL
50 mM 0.03 mL 0.15 mL 0.29 mL

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References for FMF-04-159-2

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

Ferguson et al (2019) Discovery of covalent CDK14 inhibitors with pan-TAIRE family specificity. Cell Chem.Biol. 26 804 PMID: 30930164

Ferguson et al (2019) Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14 Bioorg.Med.Chem.Letts. 29 1985 PMID: 31175010

If you know of a relevant reference for FMF-04-159-2, please let us know.

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Keywords: FMF-04-159-2, FMF-04-159-2 supplier, cyclin, dependent, kinase, Cdk, CDK, inhibitors, inhibits, CDK14, CDK16, CDK2, CDK17, CDK18, TAIRE, family, kinases, covalent, irreversible, CDK5, Subfamily, 7158, Tocris Bioscience

Citations for FMF-04-159-2

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