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FMF-04-159-2

Cat. No. 7158 Submit a Review Datasheet / COA / SDS
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Cat.No. 7158 - FMF-04-159-2 | C28H30Cl3N7O5S | CAS No. 2364489-81-4
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)
Datasheet
Citations
Reviews
Literature (4)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Technical Data

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 Data

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

Preparing Stock Solutions

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

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, Cyclin-dependent, Kinase, 7158, Tocris Bioscience

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.