Cbl-b-IN-33
Cbl-b-IN-33 is an orally active, selective inhibitor of Casitas B-lineage lymphoma-b (Cbl-b) with an IC50 of 7 nM and a Kd of 1.2 nM. Cbl-b-IN-33 inhibits non-phosphorylated E3 ubiquitin ligase Cbl-b, induces IL-2 activation in peripheral blood mononuclear cells, and exerts tumor growth inhibitory effects in a mouse colon cancer model. Cbl-b-IN-33 can be used for the research of colon cancer.
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- CAS No.: 2815221-18-0
- Formule: C29H30F5N5O
- Masse moléculaire:559.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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IL-2 |
Cbl-b-IN-33 (Compound 16) (24 h) induces IL-2 production in PBMCs with an EC50 of 0.015 μM[1].
Cbl-b-IN-33 has predicted hepatic clearance values of 14 mL/min/kg in human liver microsomes, 32 mL/min/kg in rat liver microsomes, and 66 mL/min/kg in mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:syngeneic model strain (CT26 colon cancer implantation)[1]
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Dosage:45 mg/kg (TGI 78%); 90 mg/kg (TGI 82%)
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Administration:p.o.; twice daily (45 mg/kg); once daily (90 mg/kg) for 15 days
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Result:Achieved 78% tumor growth inhibition.
Achieved 82% tumor growth inhibition.
Showed no significant body weight changes compared to untreated groups.
Chemical Information
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CAS No. 2815221-18-0
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Masse moléculaire 559.57
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Formule C29H30F5N5O
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SMILES
O=C1C2=C(C(C(F)(F)F)=CC(CNC3(C)CCC3)=C2)CN1C4=CC(C5(CC(F)(F)C5)CC6=NN=CN6C)=CC=C4
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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)