Chemical Probes logo
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
Vendors
Download

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

References

Publications

Cross References

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

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.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria