1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
    c-Met/HGFR
  3. CEP-40783

CEP-40783 (Synonyms: RXDX-106)

Cat. No.: HY-100946 Purity: 99.22%
Handling Instructions

CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.

For research use only. We do not sell to patients.

CEP-40783 Chemical Structure

CEP-40783 Chemical Structure

CAS No. : 1437321-24-8

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10 mM * 1 mL in DMSO USD 207 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 260 In-stock
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50 mg USD 780 In-stock
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100 mg USD 1170 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.

IC50 & Target

IC50: 7 nM (AXL) and 12 nM (c-Met)[1]

In Vitro

In AXL-transfected 293GT cells, CEP-40783 is 27-fold more active compared to recombinant enzyme with an IC50 value of 0.26 nM. CEP-40783 also demonstrates superior activity against c-Met in GTL-16 cells (IC50=6 nM). The increased inhibitory activity of CEP-40783 in cells could be attributed to its extended residence time on both AXL and c-Met, consistent with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 µM)[1].

In Vivo

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[1]. 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. Additionally, CEP-40783 in combination with erlotinib demonstrate superior anti-tumor efficacy compared to CEP-40783 and erlotinib single agents in the one erlotinib-sensitive model evaluated. CEP-40783 as a single agent and in combination with erlotinib are well tolerated[2].

Clinical Trial
Molecular Weight

588.56

Formula

C₃₁H₂₆F₂N₄O₆

CAS No.

1437321-24-8

SMILES

O=C(C1=CN(C(C)C)C(N(C2=CC=C(F)C=C2)C1=O)=O)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.6 mg/mL (12.91 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6991 mL 8.4953 mL 16.9906 mL
5 mM 0.3398 mL 1.6991 mL 3.3981 mL
10 mM 0.1699 mL 0.8495 mL 1.6991 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

CEP-40783RXDX-106CEP40783CEP 40783RXDX106RXDX 106TAM Receptorc-Met/HGFRTyro3AxlMerInhibitorinhibitorinhibit

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CEP-40783
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