FMF-04-159-2

Name: FMF-04-159-2
Brand: Tocris Bioscience
SKU: 7158

Tocris Bioscience, part of Bio-Techne | Catalog # 7158

COA / SDS

Potent covalent CDK14 and CDK16 inhibitor; also inhibits other TAIRE kinase family members

Key Product Details

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)
Molecular Weight:	683.01

View Full Technical Details for FMF-04-159-2

Technical Data
Citations

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
InChi Key	HZPYSAHDRSBARR-QPJJXVBHSA-N
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 for FMF-04-159-2

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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 Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14 Bioorg.Med.Chem.Letts. 2019 PMID: 31175010
Ferguson Discovery of covalent CDK14 inhibitors with pan-TAIRE family specificity. Cell Chem.Biol. 2019 PMID: 30930164