Home Cytoskeletal Signaling PAK inhibitor FRAX1036

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FRAX1036 PAK inhibitor

Cat.No.S7989

FRAX-1036 is a potent and selective PAK inhibitor with biochemical potency (Ki) of 23.3 nM and 72.4 nM against PAK1 and PAK2.
FRAX1036 PAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 518.05

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Quality Control

Batch: S798901 4-Methylpyridine]21 mg/mL]true]DMSO]Insoluble]false]Water]Insoluble]false Purity: 98.62%
98.62

Solubility

In vitro
Batch:

4-Methylpyridine : 21 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 518.05 Formula

C28H32ClN7O

 Storage (From the date of receipt)
CAS No. 1432908-05-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=NC(=CN=C4)C)Cl)NCCC5CCN(CC5)C

Mechanism of Action

Targets/IC50/Ki
PAK1
(Cell-free assay)
23.3 nM(Ki)
PAK2
(Cell-free assay)
72.4 nM(Ki)
PAK4
(Cell-free assay)
2.4 μM(Ki)
In vitro
Potent cellular inhibition of group I PAK substrate phosphorylation (MEK1-S298 and CRAF-S338) was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. Treatment of PAK1-amplified breast cancer cells with this compound results in apoptosis. And treatment of OVCAR-3 cells with this chemical results in upregulation of p53 and p21, while down-regulating cyclin B1.
In vivo
Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/25596744/

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