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FRAX1036

Catalog No. T6839 CAS 1432908-05-8

FRAX-1036 is a effective and selective PAK1 inhibitor.

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FRAX1036, CAS 1432908-05-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	FRAX-1036 is a effective and selective PAK1 inhibitor.
Targets&IC50	PAK1:23.3 nM(Ki), PAK2:72.4 nM(Ki), PAK4:2.4 μM(Ki)
In vitro	MDA-MB-175 cells,which are PAK1-amplified (MEK1-S298 and CRAF-S338) ,was observed Potent cellular inhibition at 2.5 to 5 μM concentrations of FRAX1036. PAK1-amplified breast cancer cells are treated with FRAX1036 leading to apoptosis. OVCAR-3 cells are treated with FRAX-1036 resulting in upregulation of p53 and p21, while down-regulating cyclin B1.
In vivo	KT21 are treated with Frax1036 showing slower tumor growth, while Frax1036 is unlikely to have significant blood-brain barrier permeability in mice.
Cell Research	MDA-MB175 cells are treated with increasing concentrations (0, 0.5, 1, 2.5, 5 μM) of FRAX1036 for 24 hours.
Animal Research	Pak2-deficient mice were treated by oral gavage of 30 mg/kg Frax1036.

Molecular Weight	518.06
Formula	C28H32ClN7O
CAS No.	1432908-05-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Ong CC, et al. Breast Cancer Res. 2015, 17:59. 2. Kosoff RE, et al. Blood. 2015, 125(19):21995-32005. 3. Alexander B. Koval, et al. Tetrahedron Letters. 2016, 57(3):449-451. 4. Chow HY, et al. Oncotarget. 2015, 6(4): 1981-1994.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Inhibitor Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Anti-Aging Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

Fingolimod FRAX486 PF-3758309 IPA-3 ZINC194100678 PF-3758309 hydrochloride AZ13705339 GNE 2861

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

FRAX1036 1432908-05-8 细胞骨架 PAK FRAX 1036 Inhibitor p21 activated kinases inhibit FRAX-1036 inhibitor

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