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Roblitinib | Roblitinib : Reversible-Covalent Inhibitor of FGFR4
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 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
FGFR4
  • IC50:0.9 ± 0.4 nM
  • Kd:2.9 nM
  • IC50:4.3 ± 2.5 nM
  • IC50:12 ± 6 nM
Reversible
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
KINOMEscan
Selectivity Assessment Description:
1000-fold selectivity for FGFR4 compared to the next most potent kinase inhibited (Aurora A: IC50 ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Enzyme and Receptor screens
Selectivity Assessment Description:
In enzyme and receptor screens, 84 exhibited no appreciable activity at a concentration of 10 μM aga ...

Potency
Cellular
In Vitro

FGFR4

Mode of Action: Reversible

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.0c01019

In Vivo Validations

Mouse, Rat, Dog
Dose: 1 IV, 3 PO mg/Kg (M), 0.5 IV, 3 PO mg/Kg (R), 0.1 IV, 0.3 PO mg/Kg (D)
Route of delivery: Intravenous, Oral
Plasma half life: 1.4 (M), 4.4(R), 6.5 (D) h
Systemic clearance: 28 (M), 19(R), 8 (D) mL/min/Kg

DOI Reference: 10.1021/acs.jmedchem.0c01019

Orthogonal Probes def

BLU9931

Chemical Information

Molecular Formula C25H30N8O4
SMILEs COCCNc1cc(NC(=O)N2CCCc3cc(CN4CCN(C)CC4=O)c(C=O)nc32)ncc1C#N
InChI InChI=1S/C25H30N8O4/c1-31-7-8-32(23(35)15-31)14-18-10-17-4-3-6-33(24(17)29-21(18)16-34)25(36)30-22-11-20(27-5-9-37-2)19(12-26)13-28-22/h10-11,13,16H,3-9,14-15H2,1-2H3,(H2,27,28,30,36)
Molecular weight 506.24 Da
AlogP 0.0
HBond acceptors 12
HBond donors 2
Atoms 67

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 8 Nov 2024 )
Cellular Use Rating
This is an exquisitely selective probe for FGFR4 (specific to this isoform within the FGFR family) with significant target validation and selectivity profiling across kinases and other targets, showing...
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