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eCF506 | eCF506 : ATP-competitive inhibitor of SRC
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SRC
  • IC50:0.5 nM
  • EC50:9 nM (MDA-MB-231), 70 nM (MCF7)
Inhibitor
10-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - SRC Family Members: 0.5-5.4 nM

Potency Assay Off-Target:
Radioisotope-based assay ([γ-33P] ATP) consisting of measuring 33P incorporation on the substrate (p ...
Selectivity Assessment Description:
eCF506 exclusively inhibits SRC Family Kinases. It is important to highlight that eCF506 displays ...
In Cell Selectivity Assessment

Potency: IC50 - AKT >1000 nM

Potency Assay Off-Target:
Western blot

Potency
Cellular
In Vitro

SRC

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6b00065

In Vivo Validations

Mouse, CD-1;, Zebrafish, Tg(brn3c:mGFP)
Dose: 10 mg/kg
Route of delivery: Intravenous, Oral
Plasma half life: 2.9 h
Systemic clearance: 72.3 mL/min/Kg

Reference: --

Orthogonal Probes def

DASATINIB
SARACATINIB
SU-6656

Chemical Information

Molecular Formula C26H38N8O3
SMILEs COc1cc(-c2nn(CCN3CCC(N(C)C)CC3)c3ncnc(N)c23)ccc1NC(=O)OC(C)(C)C
InChI InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
Molecular weight 510.31 Da
AlogP 3.4571
HBond acceptors 11
HBond donors 3
Atoms 75

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 13 Mar 2017 )
Cellular Use Rating
In Model Organisms
This probe is selective for SRC over ABL, but only a small number of off-target kinases (15) were screened. It appears to be equipotent against YES and is thus at least a dual inhibitor (SRC/YES). It...
by SERP
(on 5 Apr 2017 )
Cellular Use Rating
In Model Organisms
This is an ATP-competitive SRC inhibitor, selective for Src-family kinases over ABL1. In MCF7 cells, it inhibits auto-phosphorylation of SRC pY416 and its downstream substrate FAK pY861 at low nanomolar...
by SERP
(on 1 Jun 2017 )
Cellular Use Rating
IC50 values of 5 nM or less were observed for the 9 SRC family kinases included (BLK, FGR, FRK, FYN, HCK, LCK, LYN, SRC, and YES); there are two additional SRC family members, SRM and BRK, that were...
by SERP
(on 18 Apr 2018 )
Cellular Use Rating
In Model Organisms
eCF506 is a potent and selective inhibitor for the SFK family of kinases. Although it claims to be selective towards SCR proto-oncogene tyrosine-kinase, it showed the same potency than for other SFK...

Portal Comments

In a recent publication eCF506 was shown to be a type 1 1/2 inhibitor. A broader selectivity panel was used and the compound was shown to be effective in vivo.A Conformation Selective Mode of Inhibiting...

(last updated: 8 Jun 2022)

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