Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewFMF-04-159-2
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
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.
| 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets
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.
View Related Products by Target
View Related Products by Product Action
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
Citations for FMF-04-159-2
Citations are publications that use Tocris products.
Currently there are no citations for FMF-04-159-2. Do you know of a great paper that uses FMF-04-159-2 from Tocris? Please let us know.
Reviews for FMF-04-159-2
There are currently no reviews for this product. Be the first to review FMF-04-159-2 and earn rewards!
Have you used FMF-04-159-2?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
Neurodegeneration Product Guide
A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:
- Alzheimer's disease
- Parkinson's disease
- Huntington's disease
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.