| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Cbz-B3A targets the mTORC1 signaling pathway. It inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1) and p70S6 kinase (p70S6k) Thr-389. It appears to bind to ubiquilins 1, 2, and 4. By inhibiting mTORC1 signaling, it blocks cap-dependent translation.
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|---|---|
| ln Vitro |
In some human leukemia cell lines, Cbz-B3A slows cell proliferation but is not cytotoxic. Cbz-B3A has a stronger effect on 4EBP1 phosphorylation than p70S6k, when compared to rapamycin. Cbz-B3A uses ubiquitin to block mTOR. A dose-dependent reduction in [35S]methionine/cysteine incorporation into proteins is seen by Cbz-B3A, with an EC50 of roughly 3 μM and a maximal inhibition of 68% at 10 μM.
Cbz-B3A is a potent inhibitor of mTORC1 signaling. At 10 μM, it inhibits the phosphorylation of 4EBP1 and p70S6k Thr-389. It blocks translation by 68%. It slows cellular growth of some human leukemia cell lines but is not cytotoxic. It has a larger effect on the phosphorylation of 4EBP1 than p70S6k compared to rapamycin. |
| ln Vivo |
Specific in vivo activity data for Cbz-B3A is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of mTORC1 inhibition and its impact on cell growth and translation. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties.
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| Enzyme Assay |
Cbz-B3A's activity as an mTORC1 inhibitor is assessed using in vitro kinase assays or cell-based assays measuring mTORC1 activity. The compound's ability to inhibit the phosphorylation of 4EBP1 and p70S6k is assessed by Western blot analysis. Its effects on translation can be measured using assays such as polysome profiling or puromycin incorporation.
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| Cell Assay |
Cellular assays for Cbz-B3A involve treating cells with the compound and measuring mTORC1 signaling, translation, and cell growth. The phosphorylation of 4EBP1 and p70S6k is assessed by Western blot. Cell proliferation and viability are measured using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal model protocols for Cbz-B3A would involve its administration to animal models to study the role of mTORC1 in various diseases. The compound's effects on mTORC1 signaling, translation, and disease phenotypes would be assessed.
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| ADME/Pharmacokinetics |
Cbz-B3A has a molecular weight of 706.87 and a molecular formula of C35H58N6O9. Specific pharmacokinetic data is not extensively detailed in the available literature. As a small molecule inhibitor, its pharmacokinetic properties would need to be evaluated in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of Cbz-B3A has not been extensively characterized. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
Cbz-B3A (CAS# 1884710-81-9) is a research compound used to study mTORC1 signaling and its role in cell growth, translation, and cancer. It is a potent and selective inhibitor of mTORC1 signaling that inhibits 4EBP1 phosphorylation and blocks translation. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C35H58N6O9
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|---|---|
| Molecular Weight |
706.869829654694
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| Exact Mass |
706.426
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| CAS # |
1884710-81-9
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| PubChem CID |
124203916
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| Appearance |
White to off-white solid powder
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| LogP |
6.4
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
50
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C(N[C@H](C(NCCCCCCNC(=O)OCC1C=CC=CC=1)=O)CCC/N=C(\NC(=O)OC(C)(C)C)/NC(=O)OC(C)(C)C)=O)C(C)(C)C
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| InChi Key |
JGEWUYSTHGIDHO-SANMLTNESA-N
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| InChi Code |
InChI=1S/C35H58N6O9/c1-33(2,3)48-30(44)39-26(20-17-23-37-28(40-31(45)49-34(4,5)6)41-32(46)50-35(7,8)9)27(42)36-21-15-10-11-16-22-38-29(43)47-24-25-18-13-12-14-19-25/h12-14,18-19,26H,10-11,15-17,20-24H2,1-9H3,(H,36,42)(H,38,43)(H,39,44)(H2,37,40,41,45,46)/t26-/m0/s1
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| Chemical Name |
benzyl N-[6-[[(2S)-5-[bis[(2-methylpropan-2-yl)oxycarbonylamino]methylideneamino]-2-[(2-methylpropan-2-yl)oxycarbonylamino]pentanoyl]amino]hexyl]carbamate
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| Synonyms |
CbzB3A; Cbz B3A; Cbz-B3A
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.4147 mL | 7.0734 mL | 14.1469 mL | |
| 5 mM | 0.2829 mL | 1.4147 mL | 2.8294 mL | |
| 10 mM | 0.1415 mL | 0.7073 mL | 1.4147 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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