| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Cbl-b-IN-3 targets casitas B-lineage lymphoma proto-oncogene-b (Cbl-b), an E3 ubiquitin ligase that negatively regulates T cell activation. Cbl-b ubiquitinates key signaling molecules in the T cell receptor (TCR) pathway, promoting their degradation and limiting T cell activation. This negative regulation is critical for maintaining peripheral T cell tolerance and preventing autoimmune responses. By inhibiting Cbl-b with an IC50 of < 1 nM, Cbl-b-IN-3 removes this brake on T cell activation, enhancing T cell responses. This mechanism has therapeutic potential for cancer immunotherapy, where enhanced T cell activation can promote anti-tumor immunity. The compound's potent inhibition of Cbl-b makes it a valuable tool for studying T cell biology and developing immunotherapies.
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| ln Vitro |
Cbl-b-IN-3 (compound 23) stimulates T cells with anti-CD3 antibodies alone or in conjunction with anti-CD28 antibodies to produce more IL-2 [1].
In vitro, Cbl-b-IN-3 (compound 23) stimulates T cells with anti-CD3 antibodies alone or in conjunction with anti-CD28 antibodies to produce more IL-2. This demonstrates that Cbl-b inhibition enhances T cell activation and cytokine production. The compound's IC50 of < 1 nM indicates extremely potent inhibition of Cbl-b. These in vitro activities confirm that Cbl-b-IN-3 effectively blocks Cbl-b-mediated negative regulation of T cells, leading to enhanced T cell responses. The compound's ability to increase IL-2 production is consistent with its mechanism as a Cbl-b inhibitor and its potential as an immunotherapy agent. |
| ln Vivo |
In vivo studies with Cbl-b-IN-3 are not extensively documented in publicly available literature. Based on its mechanism of action as a Cbl-b inhibitor that enhances T cell activation, the compound would be expected to have anti-tumor activity in vivo by promoting anti-tumor immune responses. However, specific in vivo efficacy data (tumor models, dosing regimens, survival) have not been extensively reported. The compound's potent in vitro activity (IC50 < 1 nM) and its role as an immunotherapy agent suggest potential for in vivo applications. Researchers should consult primary literature for updated information.
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| Enzyme Assay |
In vitro enzyme assays for Cbl-b inhibition are used to characterize Cbl-b-IN-3's activity. Cbl-b is an E3 ubiquitin ligase that catalyzes the transfer of ubiquitin to target proteins. Enzyme activity can be measured using ubiquitination assays, where the compound is incubated with Cbl-b, ubiquitin, E1 and E2 enzymes, and a substrate protein. Ubiquitination is detected by Western blot or using radioactive or fluorescent labels. The compound's IC50 of < 1 nM is determined from dose-response curves. These enzyme assays are essential for characterizing the compound's potency and mechanism of action as a Cbl-b inhibitor.
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| Cell Assay |
Cell-based assays for Cbl-b-IN-3 are conducted in T cells. T cells are treated with the compound at various concentrations and stimulated with anti-CD3 antibodies alone or in conjunction with anti-CD28 antibodies. IL-2 production is measured by ELISA or flow cytometry. T cell proliferation is assessed by [³H]-thymidine incorporation or CFSE dilution. T cell activation markers (e.g., CD25, CD69) are measured by flow cytometry. These assays demonstrate that Cbl-b inhibition enhances T cell activation and cytokine production. The compound's effects on T cell function are concentration-dependent, and the IC50 for functional enhancement is consistent with its biochemical potency.
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| Animal Protocol |
In vivo animal protocols for Cbl-b-IN-3 are not extensively documented. Based on the compound's mechanism as a Cbl-b inhibitor that enhances T cell activation, typical study designs would involve administration of the compound in syngeneic tumor models (e.g., MC38 colon cancer, B16 melanoma) to assess anti-tumor efficacy. Doses would be determined from pharmacokinetic and pharmacodynamic data. Route of administration would depend on the compound's solubility and bioavailability. Endpoints would include tumor growth inhibition, survival, immune cell infiltration into tumors, and T cell activation markers. Researchers should consult primary literature for updated protocols.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cbl-b-IN-3 have not been extensively characterized. The compound has molecular weight 537.62 and molecular formula C30H34F3N5O. It is soluble in DMSO (~100 mg/mL, ~186.00 mM). Specific pharmacokinetic parameters such as half-life, Cmax, AUC, bioavailability, and tissue distribution have not been reported. Storage: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. The compound should be stored in a sealed and protected environment (e.g., under nitrogen), avoiding exposure to moisture and light.
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| Toxicity/Toxicokinetics |
Toxicology data for Cbl-b-IN-3 are limited in publicly available sources. As a potent immunomodulator that enhances T cell activation, potential toxicities include immune-related adverse events such as cytokine release syndrome, autoimmunity, and inflammation. However, comprehensive toxicology studies have not been extensively reported. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling Cbl-b-IN-3. The compound should be stored properly and disposed of in accordance with applicable regulations. Researchers should consult the material safety data sheet (MSDS) for detailed safety information.
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| References | |
| Additional Infomation |
Cbl-b-IN-3 has CAS number 2573775-59-2, molecular formula C30H34F3N5O, and molecular weight 537.62. It is a potent inhibitor of Cbl-b (E3 ubiquitin ligase) with IC50 < 1 nM. Cbl-b negatively regulates T cell activation, and its inhibition enhances T cell responses. Synonyms: NX-1607, Compound 23. Purity: ≥98%. Appearance: White to off-white powder. Solubility: DMSO ~100 mg/mL (~186.00 mM). Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Store in a sealed and protected environment, avoid moisture and light. Not approved for clinical use; for research purposes only. The compound is a valuable tool for studying T cell biology and developing cancer immunotherapies.
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| Molecular Formula |
C30H34F3N5O
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| Molecular Weight |
537.619077205658
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| Exact Mass |
537.271
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| CAS # |
2573775-59-2
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| PubChem CID |
155449671
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| Appearance |
White to off-white solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
39
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| Complexity |
894
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(=O)C2=C(C(C(F)(F)F)=CC(CN3CCC[C@H](C)C3)=C2)CN1C1=CC=CC([C@@]2(C3N(C)C=NN=3)C[C@H](C)C2)=C1
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| InChi Key |
HUOLMBXGHHSYHC-QORSJFMISA-N
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| InChi Code |
InChI=1S/C30H34F3N5O/c1-19-6-5-9-37(15-19)16-21-10-24-25(26(11-21)30(31,32)33)17-38(27(24)39)23-8-4-7-22(12-23)29(13-20(2)14-29)28-35-34-18-36(28)3/h4,7-8,10-12,18-20H,5-6,9,13-17H2,1-3H3/t19-,20?,29?/m0/s1
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| Chemical Name |
2-[3-[3-methyl-1-(4-methyl-1,2,4-triazol-3-yl)cyclobutyl]phenyl]-6-[[(3S)-3-methylpiperidin-1-yl]methyl]-4-(trifluoromethyl)-3H-isoindol-1-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~186.00 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8600 mL | 9.3002 mL | 18.6005 mL | |
| 5 mM | 0.3720 mL | 1.8600 mL | 3.7201 mL | |
| 10 mM | 0.1860 mL | 0.9300 mL | 1.8600 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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