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RBC10 (RBC-10) is a novel and potent inhibitor of the binding of Ral to its effector RALBP1 with anti-cancer activity. The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis.
| Targets |
RBC10 targets the GDP-bound form of Ral GTPases (RalA and RalB) by binding to an allosteric site adjacent to the guanine nucleotide-binding pocket, thereby inhibiting Ral activation and its downstream signaling pathways.[1]
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|---|---|
| ln Vitro |
RBC10 reduced RalA activation in J82 human bladder cancer cells stably expressing FLAG-tagged RalA, as measured by an ELISA-based RalA activity assay. The assay quantified the binding of active RalA-GTP to immobilized RalBP1. Treatment with 50 µM RBC10 for 1 hour significantly decreased RalA activation compared to DMSO control.[1]
In murine embryonic fibroblast (MEF) spreading assays, RBC10 inhibited RalA-dependent cell spreading in wild-type MEFs but not in caveolin-1 deficient (Cav1⁻/⁻) MEFs. Cells were treated with 15 µM RBC10 for 1 hour prior to spreading on fibronectin-coated coverslips.[1] |
| Cell Assay |
RalA Activity ELISA: J82 cells stably overexpressing FLAG-RalA were seeded at 800,000 cells per well in 6-well plates and incubated for 16 hours. Cells were treated with 500 µL of fresh medium containing 50 µM RBC10 or DMSO control for 1 hour at 37°C. After treatment, cells were washed with ice-cold PBS and lysed. Lysates were cleared by centrifugation and supernatants were stored at -80°C. For the ELISA, HisGrab nickel-coated 96-well plates were washed and coated with recombinant RalBP1. Cell lysates were added and incubated overnight at 4°C. Bound FLAG-RalA was detected using mouse anti-FLAG antibody followed by HRP-conjugated secondary antibody and substrate. Absorbance was measured at 450 nm.[1]
MEF Spreading Assay: Wild-type or Cav1⁻/⁻ mouse embryonic fibroblasts were starved for 24 hours, detached, and resuspended in DMEM with 0.2% serum and 0.5% methyl cellulose. Cells were held in suspension for 90 minutes at 37°C. During suspension, cells were treated with 15 µM RBC10 or DMSO for 1 hour. After treatment, cells were rinsed and plated on fibronectin-coated 24-well plates. Cells were allowed to spread for 30 minutes, then fixed and labeled for visualization. Cell spread area was quantified using ImageJ software.[1] |
| References | |
| Additional Infomation |
RBC10 was identified through a structure-based virtual screening approach targeting an allosteric site on RalA-GDP. It is one of the lead compounds (along with RBC6 and RBC8) that showed inhibitory activity against Ral GTPases in cellular assays. The compound shares a similar binding site with RBC6 and RBC8 but has distinct structural substitutions.[1]
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| Molecular Formula |
C24H25CLN2O2
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|---|---|
| Molecular Weight |
408.92
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| Exact Mass |
408.16
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| CAS # |
362503-73-9
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| PubChem CID |
22330351
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
616.3±55.0 °C at 760 mmHg
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| Flash Point |
326.5±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
661
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCC(=O)N1C(C2=C(CCCC2=O)NC3=CC=CC=C31)C4=CC=CC=C4Cl
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| InChi Key |
XERBEDAMDXRGFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25ClN2O2/c1-2-3-15-22(29)27-20-13-7-6-11-18(20)26-19-12-8-14-21(28)23(19)24(27)16-9-4-5-10-17(16)25/h4-7,9-11,13,24,26H,2-3,8,12,14-15H2,1H3
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| Chemical Name |
6-(2-chlorophenyl)-5-pentanoyl-8,9,10,11-tetrahydro-6H-benzo[b][1,4]benzodiazepin-7-one
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| Synonyms |
RBC10 RBC 10 RBC-10
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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) |
DMSO : ~125 mg/mL (~305.68 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 | 2.4455 mL | 12.2273 mL | 24.4547 mL | |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL | |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 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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