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. Nr.: 2815221-18-0
- Formel: C29H30F5N5O
- Molecular Weight:559.57
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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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. Nr. 2815221-18-0
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Molecular Weight 559.57
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)