产品资料

Tocris/FRAX 597/6029/50/50 mg

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 Technical Data Solubility Calculators Datasheets References

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
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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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: 23960073

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

Keywords: FRAX 597, supplier, FRAX597, potent, group, I, PAK, inhibits, inhibitors, p21, activated, kinase, P21-activated, Kinases, P21-activated, Kinases, Tocris Bioscience

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