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SIAIS001 | SIAIS001 : Degrader (PROTAC) of ALK
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
ALK
  • IC50:0.9 nM
  • DC50:3.9 nM
  • Dmax:70.3%
  • IC50:0.9 nM
Degrader (PROTAC)
100 nM

Selectivity

Potency
Cellular
In Vitro

ALK

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.ejmech.2021.113335

In Vivo Validations

Rat
Dose: 2 mg/Kg
Route of delivery: Intraperitoneal
Cmax: 83.45 ng/ml

DOI Reference: 10.1016/j.ejmech.2021.113335

Dose: 10 mg/Kg
Route of delivery: Oral
Cmax: 100 ng/mL
Tmax: 4h
Bioavailability: 16%

DOI Reference: 10.1016/j.ejmech.2021.113335

Chemical Information

Molecular Formula C48H51N7O4
SMILEs CCc1cc2c(cc1N1CCC(N3CCN(CCCC#Cc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O
InChI InChI=1S/C48H51N7O4/c1-4-31-26-36-38(48(2,3)45-43(44(36)57)35-13-12-30(28-49)25-39(35)50-45)27-41(31)54-19-16-33(17-20-54)53-23-21-52(22-24-53)18-7-5-6-9-32-10-8-11-34-37(32)29-55(47(34)59)40-14-15-42(56)51-46(40)58/h8,10-13,25-27,33,40,50H,4-5,7,14-24,29H2,1-3H3,(H,51,56,58)
Molecular weight 789.40 Da
AlogP 0.0
HBond acceptors 11
HBond donors 2
Atoms 110

Expert Reviews

by SERP
(on 10 Apr 2022 )
Cellular Use Rating
In Model Organisms
This ALK PROTAC is unique in being constructed from Alectinib with a phthalimide degrader functionality. The probe inhibits ALK activity in cells and convincingly induces ALK degradation, although with...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
In Model Organisms
This is a good degrader of ALK. It would have been nice if cytotoxicity assays and concentration of the hook effect would have been determined.
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