FRAX 597

Catalog #: 6029
3 Citations Datasheet

Catalog #	Availability	Size / Price	Qty
6029/10
6029/50

FRAX 597 | CAS No. 1286739-19-2 | PAK Inhibitors

1 Image

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%

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Product Details

Citations (3)

Reviews

Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:

558.1

Formula:

C₂₉H₂₈ClN₇OS

Solubility:

Soluble to 20 mM in DMSO

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

1286739-19-2

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.

Background References

FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.
Licciulli et al.
J.Biol.Chem., 2013;288:29105
FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcit.
Yeo et al.
BMC Cancer, 2016;16:24

Product Datasheets

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Citations for FRAX 597

The citations listed below are publications that use Tocris products. Selected citations for FRAX 597 include:

3 Citations: Showing 1 - 3

Structure-based design of CDC42 effector interaction inhibitors for the treatment of cancer.
Authors: Zheng Et al.
Cell Rep 2022;39:110641
PAK1 and PAK2 in cell metabolism regulation.
Authors: Pavla Et al.
J Cell Biochem 2022;123:375-389
P21-activated kinase regulates oxygen-dependent migration of vascular endothelial cells in monolayers.
Authors: Naoyuki Et al.
Cell Adh Migr 2021;15:272-284

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