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C3TD879 | C3TD879 : Type I inhibitor of CIT
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
CIT
  • IC50:12 nM
  • ΔTm:2.1 Celsius
  • Kd:0.3 nM, 9.5 nM
Type I
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
C3TD879 for profiling in the Eurofins KinaseProfiler assay against 373 human kinases and found it to ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
C3TD879 was profiled in the NCI60 panel to look for evidence of antiproliferative activity across ma ...

Potency
Cellular
In Vitro

CIT

Mode of Action: Type I

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c01807

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 4.3 h
Systemic clearance: 4.4 mL/min/kg
Cmax: 5800 nM
Area Under the Curve:: 10200 nM·h
Volume of Distribution at Steady-State: 0.91 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c01807

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 4.0 h
Cmax: 12300 nM
Area Under the Curve:: 7300 nM·h
Bioavailability: 72%

DOI Reference: 10.1021/acs.jmedchem.3c01807

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 12900 nM (plasma), 1020 nM (brain)
Area Under the Curve:: 90500 nM·h (plasma), 7710 nM·h (brain)

DOI Reference: 10.1021/acs.jmedchem.3c01807

Negative Control Compounds

C3TD879-N
Notes: C3TD879-N (cpd 59) was not able to induce thermal stabilization in biophysical assay, and did not show any binding in cellular NanoBRET experiments.
PubChem ID:

Chemical Information

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Vendors

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Expert Reviews

by SERP
(on 5 Mar 2024 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 9 Jul 2024 )
Cellular Use Rating
In Model Organisms
C3TD879 is a well-characterized selective probe for CITK. As a Type I kinase inhibitor, it binds directly to full-length human CITK in cells (Kd < 10 nM) as measured using a NanoBRET assay. C3TD879 effectively...
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