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

Cbl-b-IN-30

Cbl-b-IN-30 Chemical Structure

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Cbl-b-IN-30 Related Antibodies

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Description

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[1].

IC50 & Target[1]

IL-2

 

In Vitro

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.

Cbl-b-IN-30 Related Antibodies
Parmacokinetics
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 / / / /
In Vivo

Cbl-b-IN-30 (Compound 10) (3-30 mg/kg, p.o., daily for 15 days) inhibits tumor growth in BALB/c mice bearing CT26 syngeneic tumors[1].
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.

Animal Model: BALB/c mice bearing CT26 syngeneic tumors[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Orally administration
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.
Molecular Weight

551.61

Formula

C29H32F3N7O
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
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-30 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-30E1/E2/E3 EnzymeInterleukin RelatedE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseILADME propertiespharmacokinetic profilesCBLB inhibitorstructure-activity relationshipantitumor efficacysyngeneic mouse modelsimmune memoryCbl-bCBLBanti-PD-1 therapydownstream biomarkerstarget engagementtumor regressionSARcompound 10Inhibitorinhibitorinhibit

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