Cbl-b-IN-30
Cbl-b-IN-30 is an orally active Casitas B-lineage lymphoma-b (CBLB) inhibitor. Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM. Cbl-b-IN-30 can promote IL-2 secretion (EC50 = 187.5 nM) and enhance T cell activation. Cbl-b-IN-30 exerts antitumor activity and can induce immune memory. Cbl-b-IN-30 can be used for the research of colon cancer.
For research use only. We do not sell to patients.
- Formula: C29H32F3N7O
- Molecular Weight:551.61
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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
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IL-2 |
Cbl-b-IN-30 (Compound 10) promotes IL-2 secretion (EC50 = 187.5 nM) and enhances T cell activation in human T cells activated by anti-CD3 antibody[1].
Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM[1].
Cbl-b-IN-30 does not significantly inhibit CYP1A2/2C9/2C19/2D6/3A4 (IC50 >50 μM) and shows IC50 >30 μM for hERG, showing low risks of drug-drug interactions and cardiac toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | CL | AUC0-t | Cmax | T1/2 | F |
|---|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | p.o. | 文献审核 | / | 1074.6 ng·h/mL | 260.9 ng/mL | 2.4 h | 29.1 % |
| Mice | 30 mg/kg | p.o. | 文献审核 | / | 3536.1 ng·h/mL | 2125.7 ng/mL | 4.3 h | 52.2 % |
| Dog | 5 mg/kg | p.o. | 文献审核 | / | 159.6 ng·h/mL | 114.4 ng/mL | 1.5 h | 8.4 % |
| Rat | 1 mg/kg | i.v. | 文献审核 | 44.7 mL/min/kg | / | / | / | / |
| Mice | 1 mg/kg | i.v. | 文献审核 | 74.4 mL/min/kg | / | / | / | / |
| Dog | 1 mg/kg | i.v. | 文献审核 | 44.3 mL/min/kg | / | / | / | / |
Cbl-b-IN-30 (30 mg/kg, p.o., daily for 15 days) combined with anti-PD-1 antibody induces durable immune memory in BALB/c mice with complete tumor response, showing no tumor growth after CT26 cell rechallenge with a survival rate of 100%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice bearing CT26 syngeneic tumors[1]
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Dosage:3, 10 and 30 mg/kg
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Administration:Orally administration
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Result:Showed a TGI of 50% at 10 mg/kg without significant body weight loss.
Showed a TGI of 50% at 10 mg/kg companied with anti-PD-1 antibody.
Chemical Information
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Molecular Weight 551.61
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Formula C29H32F3N7O
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SMILES
C[C@@H]1C[C@@](C2=NN=CN2C)(C3=CC=NC(N4C=NC(C(C(F)(F)F)=CC(CN5CCC[C@@H](C5)C)=C6)=C6C4=O)=C3)C1
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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)
Cbl-b-IN-30 Related Classifications
Cat. No.: HY-179617
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- Cbl-b-IN-30
- E1/E2/E3 Enzyme
- Interleukin Related
- ADME properties
- pharmacokinetic profiles
- CBLB inhibitor
- structure-activity relationship
- antitumor efficacy
- syngeneic mouse models
- immune memory
- Cbl-b
- CBLB
- anti-PD-1 therapy
- downstream biomarkers
- target engagement
- tumor regression
- SAR
- compound 10
- Inhibitor
- inhibitor
- inhibit