FMF-04-159-2
Tocris Bioscience, part of Bio-Techne | Catalog # 7158
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
Product Description
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.Product Specifications
Molecular Weight
683.01
Formula
C28H30Cl3N7O5S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for FMF-04-159-2
For research use only
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