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A-770041 | Inhibitor of LCK
RATINGS:
Cellular Use: (3 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
LCK
  • IC50:147 nM @ 1 mM ATP
  • EC50:80 nM
Inhibitor
Potentiation of paclitaxel and doxorubicin was tested using 4 nM-10 uM in U-2OSMR and KHOSR2.
1-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
A-770041 is 300-fold selective against Fyn, the other Src-family kinase involved in T-cell signal ...

Potency
Cellular
In Vitro

LCK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2005.09.039

In Vivo Validations

Mouse, Rat
Dose: 10 mg/Kg PO, 5 mg/Kg IV
Route of delivery: Intravenous, Oral
Plasma half life: 4.7 (M), 4.1 (R) h
Systemic clearance: 1.5 (M), 0.2 (R) L/h/Kg

DOI Reference: 10.1016/j.bmcl.2005.09.039

Orthogonal Probes def

WH-4-023

Chemical Information

Molecular Formula C34H39N9O3
SMILEs COc1cc(-c2nn([C@H]3CC[C@H](N4CCN(C(C)=O)CC4)CC3)c3ncnc(N)c23)ccc1NC(=O)c1cc2ccccc2n1C
InChI InChI=1S/C34H39N9O3/c1-21(44)41-14-16-42(17-15-41)24-9-11-25(12-10-24)43-33-30(32(35)36-20-37-33)31(39-43)23-8-13-26(29(19-23)46-3)38-34(45)28-18-22-6-4-5-7-27(22)40(28)2/h4-8,13,18-20,24-25H,9-12,14-17H2,1-3H3,(H,38,45)(H2,35,36,37)/t24-,25-
Molecular weight 621.32 Da
AlogP 4.4759
HBond acceptors 12
HBond donors 3
Atoms 85

Vendors

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Expert Reviews

by SERP
(on 18 Dec 2020 )
Cellular Use Rating
In Model Organisms
This is a selective probe within the src family of RTK’s as described. Selectivity outside this family has been mentioned, but data not provided. From JPET paper: “A-770041 is 60-fold selective against...
by SERP
(on 19 Jan 2021 )
Cellular Use Rating
In Model Organisms
Initial studies involving development and medicinal chemistry were performed against purified proteins (including selectivity panels) and in vivo in rats and mice. Two later studies used this probe...
by SERP
(on 29 Mar 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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