| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
RBN-013209 targets CD38 (cluster of differentiation 38), a type II transmembrane glycoprotein with ectoenzyme activity that catalyzes the synthesis and hydrolysis of cyclic ADP-ribose (cADPR). CD38 is widely expressed on the surface of various immune cells, including B cells, plasma cells, natural killer cells, and T cells. It plays a critical role in cell adhesion, signal transduction, and calcium mobilization. Overexpression of CD38 is associated with multiple hematological malignancies, including multiple myeloma, chronic lymphocytic leukemia, and non-Hodgkin lymphoma, making it an attractive therapeutic target. By inhibiting CD38, RBN-013209 modulates immune function and reduces tumor cell proliferation.
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| ln Vitro |
In vitro, RBN-013209 demonstrates potent inhibition of CD38 with an IC50 of 0.01-0.1 μM for human CD38. The compound effectively inhibits CD38 enzymatic activity, reducing the production of cADPR and modulating intracellular calcium signaling. In cell-based assays, RBN-013209 inhibits the proliferation of CD38-expressing cancer cell lines and induces apoptosis. The compound's activity is concentration-dependent, with effective concentrations in the nanomolar to low micromolar range. Its potent CD38 inhibition makes it a valuable tool for studying CD38 biology and for developing novel immunotherapies for hematological malignancies.
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| ln Vivo |
In vivo, RBN-013209 has been studied in preclinical models of cancer, particularly in hematological malignancies such as multiple myeloma and leukemia. Administration of the compound results in significant tumor growth inhibition in mouse xenograft models. Pharmacodynamic studies confirm target engagement, showing reduced CD38 activity in tumor tissues. The compound modulates immune function, reduces inflammation, and improves survival in treated animals. Its efficacy in preclinical models supports further development as a therapeutic agent for CD38-positive cancers. However, detailed pharmacokinetic profiles and comprehensive toxicology data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro CD38 enzymatic activity assay for RBN-013209 typically uses recombinant human CD38 enzyme or membrane preparations from CD38-expressing cells. The assay is performed in 96-well plates using a fluorogenic substrate such as nicotinamide guanine dinucleotide (NGD) or a cADPR hydrolysis assay. The test compound is incubated with the enzyme at varying concentrations (typically 0.1 nM to 10 µM) for 30-60 minutes at 37°C. The reaction is initiated by adding the substrate, and fluorescence is measured at appropriate excitation/emission wavelengths. IC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., known CD38 inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, CD38-positive cancer cell lines (e.g., multiple myeloma, lymphoma, or leukemia cells) are treated with RBN-013209 at concentrations ranging from 0.01 nM to 10 µM for 24-72 hours. Cell viability is assessed using CellTiter-Glo or MTT assays. CD38 enzymatic activity is measured in cell lysates using fluorogenic substrates. Intracellular calcium levels are measured using fluorescent calcium indicators. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. For immune modulation studies, the compound's effects on cytokine production and immune cell activation are assessed. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are subcutaneously or intravenously inoculated with CD38-positive cancer cells (e.g., multiple myeloma or lymphoma cells). When tumors are established, mice are randomized into treatment groups (n=5-10 per group). RBN-013209 is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg, typically once or twice daily, for 14-28 days. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study endpoint, tumors are harvested for CD38 activity measurement, Western blot analysis, and immunohistochemistry. Pharmacodynamic studies measure CD38 inhibition and downstream signaling in tumor tissues. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of RBN-013209 have been characterized in preclinical species. The compound has a molecular weight of 384.43, a LogP of 1.2, and a tPSA of 107. Following oral administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 4-8 hours, supporting once- or twice-daily dosing. The compound distributes into tissues including tumor, liver, and kidney. Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is moderate (approximately 30-50%) due to first-pass metabolism.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of RBN-013209 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
RBN-013209 is a potent CD38 inhibitor with an IC50 of 0.01-0.1 μM for human CD38. It is used for tumor research and is useful in the treatment of cancer. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its potent CD38 inhibition makes it a valuable tool for studying CD38 biology, immune modulation, and for developing novel therapeutics for hematological malignancies.
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| Molecular Formula |
C19H24N6O3
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| Molecular Weight |
384.432263374329
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| Exact Mass |
384.19
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| CAS # |
2597933-17-8
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| PubChem CID |
155598690
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
516
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOC)C1CCC(CC1)NC(C1C2=C(C=CN2)N=C(N2C=NC=C2)N=1)=O
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| InChi Key |
VQRPLBOIYMUPNF-HDJSIYSDSA-N
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| InChi Code |
InChI=1S/C19H24N6O3/c1-27-10-11-28-14-4-2-13(3-5-14)22-18(26)17-16-15(6-7-21-16)23-19(24-17)25-9-8-20-12-25/h6-9,12-14,21H,2-5,10-11H2,1H3,(H,22,26)/t13-,14-
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| Chemical Name |
2-(1H-imidazol-1-yl)-N-((1r,4r)-4-(2-methoxyethoxy)cyclohexyl)-5H-pyrrolo[3,2-d]pyrimidine-4-carboxamide
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| Synonyms |
RBN 013209 RBN-013209 RBN013209
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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 : ~100 mg/mL (~260.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 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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