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Submit ReviewFRAX 597
Description: Potent group I PAK inhibitor
Chemical Name: 6-[2-Chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7-(8H)-one
Purity: ≥98% (HPLC)
Biological Activity for FRAX 597
FRAX 597 is a potent group I PAK inhibitor (IC50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). FRAX 597 exhibits significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC50 >10 μM for PAK4). FRAX 597 inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.
Compound Libraries for FRAX 597
FRAX 597 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 FRAX 597
| M. Wt | 558.1 |
| Formula | C29H28ClN7OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1286739-19-2 |
| PubChem ID | 70934541 |
| InChI Key | DHUJCQOUWQMVCG-UHFFFAOYSA-N |
| Smiles | CN(CC1)CCN1C2=CC=C(NC3=NC(N(CC)C(C(C4=CC=C(C5=CN=CS5)C=C4Cl)=C6)=O)=C6C=N3)C=C2 |
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 FRAX 597
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.16 | 20 |
Preparing Stock Solutions for FRAX 597
The following data is based on the product molecular weight 558.1. 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 |
|---|---|---|---|
| 0.2 mM | 8.96 mL | 44.79 mL | 89.59 mL |
| 1 mM | 1.79 mL | 8.96 mL | 17.92 mL |
| 2 mM | 0.9 mL | 4.48 mL | 8.96 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.79 mL |
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Product Datasheets for FRAX 597
References for FRAX 597
References are publications that support the biological activity of the product.
Licciulli et al (2013) FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J.Biol.Chem. 288 29105 PMID: 23960073
Yeo et al (2016) FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcit. BMC Cancer 16 24 PMID: 26774265
If you know of a relevant reference for FRAX 597, please let us know.
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Keywords: FRAX 597, FRAX 597 supplier, FRAX597, potent, group, I, PAK, inhibits, inhibitors, p21, activated, kinase, P21-activated, Kinases, 6029, Tocris Bioscience
3 Citations for FRAX 597
Citations are publications that use Tocris products. Selected citations for FRAX 597 include:
Pavla et al (2022) PAK1 and PAK2 in cell metabolism regulation. J Cell Biochem 123 375-389 PMID: 34750857
Zheng et al (2022) Structure-based design of CDC42 effector interaction inhibitors for the treatment of cancer. Cell Rep 39 110641 PMID: 35385746
Naoyuki et al (2021) P21-activated kinase regulates oxygen-dependent migration of vascular endothelial cells in monolayers. Cell Adh Migr 15 272-284 PMID: 34550057
Do you know of a great paper that uses FRAX 597 from Tocris? Please let us know.
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