2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. E1/E2/E3 Enzyme Interleukin Related
  4. 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.

For research use only. We do not sell to patients.

Cbl-b-IN-33

Cbl-b-IN-33 Chemical Structure

CAS No. : 2815221-18-0

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Cbl-b-IN-33 Related Antibodies

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Description

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[1].

IC50 & Target[1]

IL-2

 

In Vitro

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.

Cbl-b-IN-33 Related Antibodies
In Vivo

Cbl-b-IN-33 (Compound 16) (45-90 mg/kg; p.o.; once-twice daily for 15 days) produces significant tumor growth inhibition of 78% at 45 mg/kg BID and 82% at 90 mg/kg QD in a murine CT26 colon cancer syngeneic model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: syngeneic model strain (CT26 colon cancer implantation)[1]
Dosage: 45 mg/kg (TGI 78%); 90 mg/kg (TGI 82%)
Administration: p.o.; twice daily (45 mg/kg); once daily (90 mg/kg) for 15 days
Result: Achieved 78% tumor growth inhibition.
Achieved 82% tumor growth inhibition.
Showed no significant body weight changes compared to untreated groups.
Molecular Weight

559.57

Formula

C29H30F5N5O
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Cbl-b-IN-33 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cbl-b-IN-332815221-18-0E1/E2/E3 EnzymeInterleukin RelatedE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseILIL-2PBMCshuman liver microsomesc-Cblmurine colon-cancer modelsrat liver microsomesgMDCK cellsCasitas B-lineage lymphoma-bE3 ubiquitin ligase Cbl-bperipheral blood mononuclear cellsInhibitorinhibitorinhibit

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