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RILZABRUTINIB | RILZABRUTINIB : Covalent Inhibitor of BTK
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
BTK
  • IC50:1.3 nM
  • IC50:123 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The selectivity of PRN1008 was evaluated in a panel of 251 kinases. The highest levels of inhibition ...

Potency
Cellular
In Vitro

BTK

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c01170

In Vivo Validations

Rat
Dose: 2 mg/Kg IV, 20 mg/Kg PO
Route of delivery: Intravenous, Oral
Systemic clearance: 66 mL/min/kg
Cmax: 270 ng/mL
Area Under the Curve:: 622 ng·hr/mL
Bioavailability: 12.3%

DOI Reference: 10.1021/acs.jmedchem.1c01170

Negative Control Compounds

cpd 17
Notes: Biochemical BTK IC50 = 218 nM, no in Cell activity
SMILES: NC1=C2C(N(C3CN(C(C(C#N)=CC(C)C)=O)C3)N=C2C4=C(F)C=C(OC5=CC=CC=C5)C=C4)=NC=N1

Orthogonal Probes def

CGI1746
SPEBRUTINIB
PAXALISIB

Chemical Information

Molecular Formula C36H40FN9O3
SMILEs CC(C)(/C=C(\C#N)C(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3F)c3c(N)ncnc32)C1)N1CCN(C2COC2)CC1
InChI InChI=1S/C36H40FN9O3/c1-36(2,45-15-13-43(14-16-45)26-21-48-22-26)18-24(19-38)35(47)44-12-6-7-25(20-44)46-34-31(33(39)40-23-41-34)32(42-46)29-11-10-28(17-30(29)37)49-27-8-4-3-5-9-27/h3-5,8-11,17-18,23,25-26H,6-7,12-16,20-22H2,1-2H3,(H2,39,40,41)/b24-18+/t25-/m1/s1
Molecular weight 665.32 Da
AlogP 4.4153800000000025
HBond acceptors 12
HBond donors 2
Atoms 89

Vendors

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Expert Reviews

by SERP
(on 9 Jul 2026)
Cellular Use Rating
In Model Organisms
Further measurements on cysteine/GSH can be used to assess intrinsic warhead reactivity
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