FRAX597

Alias: FRAX597; FRAX-597; FRAX 597
Cat No.:V1595 Purity: ≥98%
FRAX597 (FRAX-597;FRAX 597) is a novel, potent and ATP-competitive inhibitor of group I PAKs (p21-activated Kinases) with potential anticancer activity.
FRAX597 Chemical Structure CAS No.: 1286739-19-2
Product category: PAK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

FRAX597 (FRAX-597; FRAX 597) is a novel, potent and ATP-competitive inhibitor of group I PAKs (p21-activated Kinases) with potential anticancer activity. It inhibits PAK1, PAK2, and PAK3 with IC50s of 8 nM, 13 nM, and 19 nM, respectively. FRAX597 inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. FRAX597 inhibits the proliferation of NF2-deficient schwannoma cells in culture and displayed potent anti-tumor activity in vivo, impairing schwannoma development in an orthotopic model of NF2. These studies identify a novel class of orally available ATP-competitive Group I PAK inhibitors with significant potential for the treatment of NF2 and other cancers.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
It is found that FRAX597 is a strong, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with the following biochemical IC50 values: PAK2 IC50 = 13 nM, PAK3 IC50 = 19 nM, and PAK1 IC50 = 8nM. PAK4, a member of group II PAKs, has an IC50 of greater than 10 μM. FRAX597 exhibits a notable (>80% inhibition) inhibitory ability at 100 nM towards YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). Using the Kinase Glo Assay with 20 nM protein and 1 μM ATP, FRAX597 demonstrated an IC50 value of 48 nM against PAK1 wild type, whereas IC50 values against PAK1 mutants V342F and V342Y exceed 3 μM and 2 μM, respectively[1].
ln Vivo
A comparison between the tumor growth rates of FRAX597-treated and control mice shows that the tumor growth rate in the animals in the two cohorts is much slower. The animals are slaughtered and the tumors are removed and weighed following a 14-day course of treatment. When compared to the control group, the FRAX597-treated cohort exhibits a considerably lower average tumor weight [1].
Animal Protocol
Dissolved in 10% (PEG400:Tween-80:PVP-K30, 90:5:5), 15% Vitamin E-TPGS, 75% of hydroxypropylcellulose (0.5%) in 50 mM citrate buffer (pH 3.0); 90 mg/kg/day; p.o. administration
SCID mice with orthotopic meningioma model
References
[1]. Licciulli S, et al. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H28CLN7OS
Molecular Weight
558.10
CAS #
1286739-19-2
SMILES
ClC1C([H])=C(C2=C([H])N=C([H])S2)C([H])=C([H])C=1C1=C([H])C2=C([H])N=C(N=C2N(C([H])([H])C([H])([H])[H])C1=O)N([H])C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H]
InChi Key
DHUJCQOUWQMVCG-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H28ClN7OS/c1-3-37-27-20(14-24(28(37)38)23-9-4-19(15-25(23)30)26-17-31-18-39-26)16-32-29(34-27)33-21-5-7-22(8-6-21)36-12-10-35(2)11-13-36/h4-9,14-18H,3,10-13H2,1-2H3,(H,32,33,34)
Chemical Name
6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one
Synonyms
FRAX597; FRAX-597; FRAX 597
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 14 mg/mL (25.1 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7918 mL 8.9590 mL 17.9179 mL
5 mM 0.3584 mL 1.7918 mL 3.5836 mL
10 mM 0.1792 mL 0.8959 mL 1.7918 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • FRAX597

  • FRAX597

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