Home Protein Tyrosine Kinase Axl inhibitor - Tyro3 inhibitor - Mertk inhibitor - c-Met inhibitor CEP-40783 (RXDX-106) For research use only.

CEP-40783 (RXDX-106)

CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.

CEP-40783 (RXDX-106) Chemical Structure

CEP-40783 (RXDX-106) Chemical Structure

CAS No. 1437321-24-8

Purity & Quality Control

CEP-40783 (RXDX-106) Related Products

Biological Activity

Description CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
Targets
Axl [2]
(Cell-free assay)		 c-Met [2]
(Cell-free assay)		 Tyro3 [2]
(Cell-free assay)		 MER [2]
(Cell-free assay)		 Tyro3 [2]
(Cell-free assay)		 Click to View More Targets
7 nM 12 nM 19 nM 29 nM 29 nM
In vitro
In vitro RXDX-106 inhibits TAM and c-MET phosphorylation in vitro. This inhibition of TAM and c-MET activation in vitro is accompanied by a decrease in downstream MAPK and PI3K signaling and cell viability[1]. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells[2].
Cell Research Cell lines 3T3 cells
Concentrations 0.25, 1, 2.5, 10, 25, 100, 250 nM
Incubation Time 30 min
Method

3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or RXDX-106 for 30 minutes, and receptor phosphorylation is monitored. 
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MerTK / MerTK / p-ERK / ERK / p-AKT / AKT 29285287
In Vivo
In vivo RXDX-106 could inhibit tumors harboring activating TAM gene fusions and affect the TAM-expressing tumor microenvironment to result in a global anti-cancer environment[1].
Animal Research Animal Models SCID Beige mice
Dosages 30 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 588.56 Formula

C31H26F2N4O6
CAS No. 1437321-24-8 SDF Download CEP-40783 (RXDX-106) SDF
Smiles CC(C)N1C=C(C(=O)N(C1=O)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C5C=C(C(=CC5=NC=C4)OC)OC)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (16.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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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