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Chemical Structure| 1437321-24-8 Chemical Structure| 1437321-24-8

Structure of CEP-40783
CAS No.: 1437321-24-8

Chemical Structure| 1437321-24-8

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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. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells.

Synonyms: RXDX-106

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Product Details of CEP-40783

CAS No. :1437321-24-8
Formula : C31H26F2N4O6
M.W : 588.56
SMILES Code : 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
Synonyms :
RXDX-106
MDL No. :MFCD28502441
InChI Key :FKCWHHYUMFGOPY-UHFFFAOYSA-N
Pubchem ID :71576419

Safety of CEP-40783

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CEP-40783

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Ba/F3 cells 100 nM 72 hours Screening for drugs that inhibit MET D1228A/Y secondary mutations, CEP-40783 showed inhibitory effects PMC9188708
Calu1 5 μM 72h PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC8983558
Calu1 1 μM 4 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC8983558
H1299 5 μM 72h PMC8983558
H1299 1 μM 4 hours PMC8983558
H1299 100 nM 30 min PMC8983558
Calu1 100 nM 30 min PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC8983558
NCI-H1792 1 μM 6 and 24 hours Analysis of signaling responses following KRASG12C inhibition identified FGFR1 signaling activation as an adaptive resistance mechanism in H1792 cells. PMC9940280
Calu1 1 μM 6 and 24 hours PD0166285 significantly reduced the number and size of cell colonies and showed anti-tumor effects through CCK8 assay. PMC9940280
NCI-H358 1 μM 6 and 24 hours Analysis of signaling responses following KRASG12C inhibition identified HER2/HER3 signaling activation as an adaptive resistance mechanism in H358 cells. PMC9940280

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Mice and monkeys Injection 28 days Combination of CEP-40783 and BEZ235 more effectively inhibits pAxl and pAkt, inhibits tumor cell proliferation, and promotes cell apoptosis PMC8933087

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03454243 Advanced or Metastatic Solid T... More >>umors Less << EARLY_PHASE1 TERMINATED 2018-06-05 START, San Antonio, Texas, 782... More >>29, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.50mL

1.70mL

0.85mL

16.99mL

3.40mL

1.70mL

References

 

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