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Cat. No. M8928
CEP-40783 Structure


Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
25mg USD 330  USD330 In stock
50mg USD 420  USD420 In stock
100mg USD 600  USD600 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CEP-40783 (RXDX-106) is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In 3/5 (60%) of the tumor models, CEP-40783 shows in vivo efficacy, including tumor regressions, significantly superior to that achieved with an optimal regimen of paclitaxel. In 4/4 (100%) of the erlotinib-insensitive tumor models, CEP-40783 demonstrates significant efficacy (66 to 118% TGI) compared to the control group at the 30 mg/kg dose.

Cell Experiment
Cell lines 3T3 cells
Preparation method 3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or CEP-40783 for 30 minutes, and receptor phosphorylation is monitored.
Concentrations 0.25, 1, 2.5, 10, 25, 100, 250 nM
Incubation time 30 min
Animal Experiment
Animal models SCID Beige mice
Dosages 30 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 588.56
Formula C31H26F2N4O6
CAS Number 1437321-24-8
Purity >98%
Solubility DMSO 8 mg/mL
Storage at -20°C
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Abmole Inhibitor Catalog

Keywords: CEP-40783, RXDX-106 supplier, c-Met, inhibitors

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