FRAX 597

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Cat.No. 6029 - FRAX 597 | C29H28ClN7OS | CAS No. 1286739-19-2
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)
Datasheet
Citations
Literature

Biological Activity

Potent group I PAK inhibitor (IC50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). 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). Inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.16 20

Preparing Stock Solutions

The following data is based on the product molecular weight 558.1. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.79 mL 8.96 mL 17.92 mL
5 mM 0.36 mL 1.79 mL 3.58 mL
10 mM 0.18 mL 0.9 mL 1.79 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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: 3960073

Yeo et al (2016) FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine. BMC Cancer 16 24 PMID: 26774265


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Literature in this Area

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Pathways for FRAX 597

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