Cbl-b-IN-34
Cbl-b-IN-34 is an orally active and selective Cbl-b inhibitor with a human Kd of 2.4 nM. Cbl-b-IN-34 induces T-cell activation. Cbl-b-IN-34 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2925237-58-5
- Formula: C29H32F3N5O2
- Molecular Weight:539.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Cbl-b-IN-34 (Compound 33) binds purified Cbl-b with a Kd of 2.4 nM and exhibits 14-fold selectivity for Cbl-b over c-Cbl in SPR assays[1].
Cbl-b-IN-34 induces IL-2 production in PBMCs with an EC50 of 78 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (1×105 CT26 was injected to establish a xenograft model)[1]
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Dosage:45 mg/kg; 90 mg/kg; 200 mg/kg
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Administration:p.o.; QD or BID for 7 days
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Result:Exhibited no efficacy for 45 mg/kg BID or 90 mg/kg QD dose.
Achieved TGIs of 131% for 90 mg/kg BID dose and 145% for 200 mg/kg QD dose, respectively.
Caused no body weight loss or
animal death at all doses.
Chemical Information
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CAS No. 2925237-58-5
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Molecular Weight 539.59
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Formula C29H32F3N5O2
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SMILES
O=C1N(C2=CC=CC([C@@]3(C4=NN=CN4C)C[C@@H](OC)C3)=C2)CC5=C1C=C(CNC6(C)CCC6)C=C5C(F)(F)F
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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)