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: 1437321-24-8

Selleck's CEP-40783 (RXDX-106) has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.57%
99.57

CEP-40783 (RXDX-106) Related Products

Choose Selective Axl Inhibitors

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy CEP-40783 (RXDX-106) | CEP-40783 (RXDX-106) supplier | purchase CEP-40783 (RXDX-106) | CEP-40783 (RXDX-106) cost | CEP-40783 (RXDX-106) manufacturer | order CEP-40783 (RXDX-106) | CEP-40783 (RXDX-106) distributor