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TL13-112 | TL13-112 : Degrader (PROTAC) of ALK
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ALK
  • IC50:0.6 nM
  • DC50 @ 16h:10 nM (H3122); 40 nM (K-299); 50 nM (Kelly)
Degrader (PROTAC)
250 nM, up to 1 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Degradation of targets other than ALK, including PTK2, FER, RPS6KA1, and Aurora A, was measured a ...

Potency
Cellular
In Vitro

ALK

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.7b01655

Negative Control Compounds

TL13-110

Orthogonal Probes def

Ceritinib
Brigatinib
CH5424802

Chemical Information

Molecular Formula C49H60ClN9O10S
SMILEs Cc1cc(Nc2ncc(Cl)c(Nc3ccccc3S(=O)(=O)C(C)C)n2)c(OC(C)C)cc1C1CCN(CCOCCOCCNC(=O)CNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
InChI InChI=1S/C49H60ClN9O10S/c1-29(2)69-40-26-34(31(5)25-38(40)55-49-53-27-35(50)45(57-49)54-36-10-6-7-12-41(36)70(65,66)30(3)4)32-15-18-58(19-16-32)20-22-68-24-23-67-21-17-51-43(61)28-52-37-11-8-9-33-44(37)48(64)59(47(33)63)39-13-14-42(60)56-46(39)62/h6-12,25-27,29-30,32,39,52H,13-24,28H2,1-5H3,(H,51,61)(H,56,60,62)(H2,53,54,55,57)
Molecular weight 1001.39 Da
AlogP 5.737020000000005
HBond acceptors 19
HBond donors 5
Atoms 130

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Expert Reviews

by SERP
(on 23 Apr 2024 )
Cellular Use Rating
The strong point of the publication revealing TL13-112 is the broad profiling of the PROTAC against many cell lines across range of different time points and concentrations. Also the mechanism of action...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
.Care should be taken that at concentrations higher than the recommended 10 nM, other kinases such as RPS6KA3 might be degraded, judged from the proteomics profile.
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