Cbl-b-IN-16
Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity.
For research use only. We do not sell to patients.
- Formula: C26H27F3N6O
- Molecular Weight:496.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: Cbl-b (30 nM)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | EC50 |
0.23 μM
Compound: 31
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Induction of IL-2 production in human T cells
Induction of IL-2 production in human T cells
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[PMID: 38227216] |
Cbl-b-IN-16 regulates the TCR signaling through inihibiting the autoubiquitination of Cbl-b and the ubiquitin transfer to Zap-70, with IC50s of 63 nM and 84 nM, respectively[1].
Cbl-b-IN-16 (5 μM, 20 min) inhibits the phosphorylation of Cbl-b via spleen tyrosine kinase (SYK)[1].
Cbl-b-IN-16 inhibition enhances the TCR signaling and thereby upregulates the levels of pPLCγ1 in Hu-T-cells with an EC50 of 0.61 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis of Cbl-b-IN-16 in CD1 mice and Wistar Han rats[1]
| species | route | Dose (mg/kg) | CL (mL/min/kg) | Vss (L/kg) | T1/2 (h) | Cmax (μg/mL) | Tmax (h) | AUCinf (μg·h/mL) | F (%) | Calculated EHc |
| mouse | iv | 0.5 | 100 | 1.3 | 0.3 | - | - | - | - | 0.66 |
| mouse | po | 1.0 | - | - | - | 0.035 | 0.083 | 0.030 | 19 | - |
| rat | iv | 0.5 | 55 | 1.6 | 0.45 | - | - | - | - | 0.76 |
| rat | po | 1.0 | - | - | - | 0.021 | 0.75 | 0.046 | 15 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 496.53
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Formula C26H27F3N6O
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SMILES
O=C1C(C2=CC=CC([C@@]3(C4=NN=CN4C)C[C@H](C)C3)=C2)=CC(C(F)(F)F)=CN1[C@H](C5=CN(C)N=C5)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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