Home Cytoskeletal Signaling PAK inhibitor FRAX1036 For research use only.

FRAX1036

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 Chemical Structure

FRAX1036 Chemical Structure

CAS: 1432908-05-8

Selleck's FRAX1036 has been cited by 5 publications

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
PAK1 [1]
(Cell-free assay)		 PAK2 [1]
(Cell-free assay)		 PAK4 [1]
(Cell-free assay)
23.3 nM(Ki) 72.4 nM(Ki) 2.4 μM(Ki)
In vitro
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 FRAX1036 results in apoptosis[1]. And treatment of OVCAR-3 cells with FRAX-1036 results in upregulation of p53 and p21, while down-regulating cyclin B1[3].
Cell Research Cell lines MDA-MB175 cells
Concentrations 0, 0.5, 1, 2.5, 5 μM
Incubation Time 24 h
Method

MDA-MB175 cells are treated with increasing concentrations of FRAX1036 for 24 hours. Cell lysates are immunoblotted with antibodies against biomarkers involved in PAK1 effector and survival signaling.
In Vivo
In vivo Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice[4].
Animal Research Animal Models Pak2-deficient mice
Dosages 30 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 518.05 Formula

C28H32ClN7O
CAS No. 1432908-05-8 SDF Download FRAX1036 SDF
Smiles CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=NC(=CN=C4)C)Cl)NCCC5CCN(CC5)C
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 21 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh 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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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