ICB-7
ICB-7 is an orally active ILT3/LILRB4 inhibitor with a Kd of 156 nM for hILT3 and a Kd of 262 nM for mouse ILT3. ICB-7 reduces SCG2-induced phosphorylation of SHP1, SHP2, and STAT3. In a co-culture model, ICB-7 restores IFN-γ and IL-2 secretion and decreases cell viability under SCG2 stimulation. In a syngeneic cancer model, ICB-7 inhibits tumor progression and reduces final tumor weight. ICB-7 can be used for research on colorectal cancer and acute myeloid leukemia.
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- CAS No.: 920836-30-2
- Formule: C22H21ClN4O2S
- Masse moléculaire:440.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
hILT3 156 |
mILT3 262 nM (Kd) |
STAT3 |
IL-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
289 nM
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Target engagement against human ILT3 in CHO cells stably expressing ILT3/LILRB4 assessed by cellular thermal shift assay (CETSA) with 60 min incubation and thermal challenge at 51 °C for 3 min.
Target engagement against human ILT3 in CHO cells stably expressing ILT3/LILRB4 assessed by cellular thermal shift assay (CETSA) with 60 min incubation and thermal challenge at 51 °C for 3 min.
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42702174 |
| THP-1 | IC50 |
302 nM
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Inhibition of SCG2-induced SHP1 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
Inhibition of SCG2-induced SHP1 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
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42702174 |
| THP-1 | IC50 |
285 nM
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Inhibition of SCG2-induced SHP2 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
Inhibition of SCG2-induced SHP2 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
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42702174 |
| THP-1 | IC50 |
196 nM
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Inhibition of SCG2-induced STAT3 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
Inhibition of SCG2-induced STAT3 phosphorylation in THP-1-derived macrophage-like cells after 1 h stimulation at 37 °C by ELISA.
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42702174 |
| WI-38 | IC50 |
>100 μM
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Cytotoxicity against human WI-38 lung fibroblasts assessed at concentrations up to 100 µM.
Cytotoxicity against human WI-38 lung fibroblasts assessed at concentrations up to 100 µM.
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42702174 |
| HS27 | IC50 |
>100 μM
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Cytotoxicity against human HS27 stromal cells assessed at concentrations up to 100 µM.
Cytotoxicity against human HS27 stromal cells assessed at concentrations up to 100 µM.
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42702174 |
In Vitro
ICB-7 (60 min) engages endogenous ILT3 in CHO-ILT3 cells with EC50 289 nM in CETSA[1].
ICB-7 (0.0001-10 μM; 2 h) disrupts the ILT3-SCG2 interaction with IC50 694 nM in the TR-FRET competition assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1-derived macrophage-like cells
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Concentration:PMA 100 nM; SCG2 100 ng/mL; ICB-7 at increasing concentrations
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Incubation Time:48 h (PMA); 24 h (resting); 1 h (stimulation at 37 °C)
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Result:Dose-dependently reduced SCG2-driven phosphorylation: p-SHP1 IC50 = 302 nM; p-SHP2 IC50 = 285 nM; p-STAT3 IC50 = 196 nM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (immunocompetent)[1]
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Dosage:25 mg/kg
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Administration:p.o. (oral gavage); once daily; 21 days
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Result:Inhibited CT26 tumor progression compared with vehicle controls, with divergence of tumor growth kinetics throughout the study period.
Final tumor weights collected at study termination were substantially reduced relative to controls.
Increased intratumoral IFN-γ and IL-2 levels compared with vehicle control tumors.
- Kinase activity and phosphorylation assays
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Neuron-Astrocyte Co-culture
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 920836-30-2
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Masse moléculaire 440.95
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Formule C22H21ClN4O2S
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SMILES
COC1=C(C=C(C=C1)Cl)NC(CN(CC2=C(N=C3SC=CN32)C4=CC=CC=C4)C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ICB-7 Related Classifications
HY-189933 Related Classifications
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