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UNC-8969 | UNC-8969 : Inhibitor of MERTK, AXL
RATINGS:
Cellular Use: (0 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
MERTK
  • IC50:1.1 nM
  • EC50:20.7
  • EC50:146 nM
AXL
  • IC50:5.3 nM
  • EC50:103 nM
  • EC50:83 nM
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity of UNC8969 against other members of the kinome was evaluated in a Off-chip Mobility ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity against TYRO3 was confirmed using NanoBRET EC50 >4 uM

Potency
Cellular
In Vitro

MERTK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.4c00148

AXL

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.4c00148

In Vivo Validations

Mouse
Dose: 3 mg/Kg
Route of delivery: Intravenous
Plasma half life: 6.3 h
Systemic clearance: 38.3 mL/min/kg
Cmax: 5293 ng/mL
Area Under the Curve:: 1288 h·ng/mL

DOI Reference: 10.1021/acs.jmedchem.4c00148

Dose: 3 mg/Kg
Route of delivery: Oral
Plasma half life: 1.9 h
Cmax: 14.4 ng/mL
Area Under the Curve:: 54.2 h·ng/mL
Bioavailability: 4.2 %

DOI Reference: 10.1021/acs.jmedchem.4c00148

Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 7.3 h
Systemic clearance: 42.7 mL/min/kg
Cmax: 4085 ng/mL
Area Under the Curve:: 1916 h·ng/mL

DOI Reference: 10.1021/acs.jmedchem.4c00148

Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 7.0 h
Cmax: 890 ng/mL
Area Under the Curve:: 3028 h·ng/mL
Bioavailability: 81 %

DOI Reference: 10.1021/acs.jmedchem.4c00148

Chemical Information

Molecular Formula C29H41N7O3
SMILEs CCN(CC)CCNC(=O)[C@H]1CC[C@H](NC(=O)c2cnc3nc2Nc2ccc(C)c(c2)OC/C=C\CN3)CC1
InChI InChI=1S/C29H41N7O3/c1-4-36(5-2)16-15-30-27(37)21-9-12-22(13-10-21)34-28(38)24-19-32-29-31-14-6-7-17-39-25-18-23(11-8-20(25)3)33-26(24)35-29/h6-8,11,18-19,21-22H,4-5,9-10,12-17H2,1-3H3,(H,30,37)(H,34,38)(H2,31,32,33,35)/b7-6-/t21-,22-
Molecular weight 535.33 Da
AlogP 3.635720000000001
HBond acceptors 10
HBond donors 4
Atoms 80

References

Publications

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Expert Reviews

No SERP comments found for UNC-8969

Probe UNC-8969 is in the process of SERP review.

Please continue to check back for new reviews and commentary.