| Size | Price | Stock | Qty |
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| Targets |
Caspase-1 RIPK2
cRIPGBM chloride targets receptor-interacting protein kinase 2 (RIPK2), a serine/threonine kinase involved in inflammatory signaling and cell death pathways. By binding to RIPK2, cRIPGBM chloride acts as a molecular switch that shifts RIPK2 signaling towards apoptosis. The compound induces caspase 1-dependent apoptosis. cRIPGBM chloride is an orally active pro-apoptotic derivative with antitumor activity. |
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| ln Vitro |
Time-dependently, cRIPGBM(chloride) (0.25 μM; 0-24 hours) stimulates PARP cleavage and caspases 1, 9, and 7 [1]. For 24 hours, CBM-1 GBM CSCs are exposed to 0.125 μM or 0.25 μM of cRIPGBM(chloride) which causes caspase 1-mediated apoptosis[1].
In vitro studies demonstrate that cRIPGBM chloride is a pro-apoptotic derivative that targets RIPK2 to induce caspase 1-dependent apoptosis. The compound has antitumor activity. cRIPGBM chloride is generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). No detailed IC50 or EC50 values have been published in the available literature. |
| ln Vivo |
In a mouse model with intracranial xenografts of patient-derived GBM CSCs, cRIPGBM chloride (50 mg/kg; oral; twice daily for 5 weeks) suppresses tumor growth [1].
In vivo, cRIPGBM chloride is orally active and has antitumor activity. The compound targets RIPK2 to induce caspase 1-dependent apoptosis. cRIPGBM chloride is a pro-apoptotic derivative that can be used for the study of glioblastoma and other cancers. Its oral bioavailability makes it suitable for oral administration in animal models. |
| Enzyme Assay |
The RIPK2 binding activity of cRIPGBM chloride can be assessed using in vitro binding assays. In a typical assay, recombinant RIPK2 protein is incubated with varying concentrations of cRIPGBM chloride. The binding affinity is measured using surface plasmon resonance, isothermal titration calorimetry, or fluorescence polarization assays. The compound's ability to induce caspase 1-dependent apoptosis can be assessed using cell-based apoptosis assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: GBM-1 GBM CSCs Tested Concentrations: 50 nM, 100 nM, 125 nM, 250 nM, and 500 nM Incubation Duration: 3 h, 6 h, 12 h, and 24 h Experimental Results: Had the ability to regulate RIPK2 to act as a prosurvival or proapoptotic molecule. Dramatically decreased RIPK2 binding to cIAP2 in a dose-dependent manner. The cellular activity of cRIPGBM chloride is assessed using glioblastoma or other cancer cell lines. Cells are treated with varying concentrations of cRIPGBM chloride. Apoptosis is assessed by measuring caspase-1 activation, annexin V/propidium iodide staining, or detecting cleaved caspase-1 and its substrates. Cell viability is measured using MTT or CellTiter-Glo assays. The compound's ability to inhibit tumor cell growth is assessed. |
| Animal Protocol |
Animal/Disease Models: Orthotopic intracranial xenograft model in mouse[1]
Doses: 50 mg/kg Route of Administration: PO; twice (two times) daily, 8 h apart, starting at day 7 postinjection; last for 5 weeks Experimental Results: Monitored by Fluorescence Tomography System. diminished the tumor signal, as well as tumor size. cRIPGBM chloride has been evaluated in animal models of glioblastoma. In these studies, the compound is administered orally. Tumor growth is assessed by measuring tumor volumes. The compound has antitumor activity. Its oral bioavailability makes it suitable for oral administration in animal models. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for cRIPGBM chloride. The compound is orally active, indicating favorable oral bioavailability. The compound has a molecular weight of 446.90 and a molecular formula of C26H20ClFN2O2. It has a purity of ≥98%. Further studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for cRIPGBM chloride. As a RIPK2-targeting pro-apoptotic agent, the compound may have on-target effects on RIPK2-mediated inflammatory and cell death pathways in normal tissues. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
cRIPGBM chloride (CAS# 2361988-77-2) is an orally active, pro-apoptotic derivative that targets receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. It is generated from glioblastoma multiforme (GBM) cancer stem cells and has antitumor activity. The compound acts as a molecular switch that binds to RIPK2 and induces caspase 1-dependent cell death. The molecular formula is C26H20ClFN2O2 and molecular weight is 446.90.
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| Molecular Formula |
C26H20CLFN2O2
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|---|---|
| Molecular Weight |
446.900609016418
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| Exact Mass |
446.119
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| CAS # |
2361988-77-2
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| Related CAS # |
cRIPGBM;2361988-76-1
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| PubChem CID |
156024495
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C=CC(F)=CC=1)[N+]1=C(N(CC2C=CC=CC=2)C2C(C3=CC=CC=C3C(=O)C1=2)=O)C.[Cl-]
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| InChi Key |
IHNGETPFBJHWFE-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C26H20FN2O2.ClH/c1-17-28(15-18-7-3-2-4-8-18)23-24(29(17)16-19-11-13-20(27)14-12-19)26(31)22-10-6-5-9-21(22)25(23)30;/h2-14H,15-16H2,1H3;1H/q+1;/p-1
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| Chemical Name |
3-benzyl-1-[(4-fluorophenyl)methyl]-2-methylbenzo[f]benzimidazol-3-ium-4,9-dione;chloride
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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, avoid exposure to moisture. |
| 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 : 25 mg/mL (55.94 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 | 2.2376 mL | 11.1882 mL | 22.3764 mL | |
| 5 mM | 0.4475 mL | 2.2376 mL | 4.4753 mL | |
| 10 mM | 0.2238 mL | 1.1188 mL | 2.2376 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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