| 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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| 100mg |
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| Other Sizes |
| Targets |
RO 90-7501 targets multiple cellular pathways and proteins. It inhibits the assembly of amyloid β42 (Aβ42) fibrils, reducing Aβ42-induced cytotoxicity with an EC50 of 2 μM. It inhibits ATM phosphorylation and DNA repair, and suppresses ATM and its downstream proteins, including H2AX, Chk1, and Chk2, after irradiation. RO 90-7501 also inhibits protein phosphatase 5 (PP5) through a novel, TPR-dependent mechanism, and selectively enhances TLR3 and RLR ligand-induced IFN-β gene expression and antiviral responses.
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| ln Vitro |
Ro 90-7501 markedly increased radiosensitivity in comparison to ME-180 and HeLa control cells. After radiation, Ro 90-7501 dramatically promotes apoptosis and impairs the cell cycle. Following radiation exposure, Ro 90-7501 prevents ATM and its downstream proteins—including H2AX, Chk1, and Chk2—from becoming phosphorylated [1]. While RO 90-7501 alone has no effect on the activity of the IFN-β and NFκB promoters, it dramatically amplifies the activation of the IFN-β promoter produced by poly I:C and dose-dependently suppresses the activation of the NFκB. The antiviral activity of poly I:C can be markedly increased by treating cells with RO 90-7501 [2].
In vitro, RO 90-7501 inhibits Aβ42 fibril assembly with an EC50 of 2 μM in cytotoxicity reduction assays. It inhibits ATM phosphorylation and DNA repair, and suppresses ATM and its downstream proteins, such as H2AX, Chk1, and Chk2, after irradiation. RO 90-7501 also inhibits PP5 in a TPR-dependent manner, and selectively enhances TLR3 and RLR ligand-induced IFN-β gene expression and antiviral responses. It has significant radiosensitizing effects on cervical cancer cells. |
| ln Vivo |
Treatment with Ro 90-7501 (5 μg/g; intraperitoneal injection; daily; for 21 days; female BALB/c nude mice) markedly reduced tumor volume and delayed tumor progression [1].
In vivo, RO 90-7501 has demonstrated significant radiosensitizing effects in tumor growth delay assays using BALB/c-nu mice. The combination of irradiation with RO 90-7501 showed significant radiosensitizing effects in tumor growth delay assays. RO 90-7501 significantly increased apoptosis and impaired cell cycle after irradiation. These in vivo studies confirm its potential as a radiosensitizer in cancer therapy. |
| Enzyme Assay |
Cell-free assays for RO 90-7501 can measure its inhibition of Aβ42 fibril assembly using Thioflavin T fluorescence or electron microscopy to monitor fibril formation. Its inhibition of PP5 can be assessed using phosphatase activity assays with purified PP5 and a substrate, in the presence of varying concentrations of RO 90-7501. Its ability to inhibit ATM phosphorylation can be studied using kinase activity assays with recombinant ATM. These assays confirm its multifunctional inhibitory profile.
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| Cell Assay |
Cellular assays for RO 90-7501 are performed using various cell lines, including HeLa cervical cancer cells. Cells are treated with varying concentrations of RO 90-7501, and cell viability is measured by MTT or clonogenic survival assays. Apoptosis is evaluated by annexin V staining or caspase activity assays. ATM phosphorylation and downstream signaling are assessed by Western blotting. IFN-β production is measured by ELISA. These assays confirm its functional activities.
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| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (8weeks old) with HeLa cells under irradiation[1]
Doses: 5 μg/g Route of Administration: intraperitoneal (ip)injection; daily; for 21 days Experimental Results: Tumor growth was Dramatically delayed in the combination group. Tumor volume was also Dramatically diminished in the irradiation group. In vivo animal experiments for RO 90-7501 are conducted in mouse models, such as BALB/c-nu mice bearing tumor xenografts. Animals are treated with RO 90-7501 in combination with irradiation. Tumor growth delay is assessed. Apoptosis and cell cycle impairment are evaluated in tumor tissues. ATM phosphorylation and downstream protein levels are assessed by Western blotting. These studies confirm its in vivo radiosensitizing efficacy. |
| ADME/Pharmacokinetics |
RO 90-7501 has a molecular weight of 340.39 g/mol and a molecular formula of C20H16N6. Its chemical name is 2'-(4-Aminophenyl)-[2,5'-bi-1H-benzimidazol]-5-amine. It has a purity of ≥98% (HPLC) and is a brown crystalline solid. It is soluble in DMSO (~20 mg/mL) but insoluble in water. It should be stored at -20°C for long-term storage.
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| Toxicity/Toxicokinetics |
The toxicological profile of RO 90-7501 has not been extensively characterized. It is classified as an irritant (Xi) with hazard statements H315-H319-H335. It requires personal protective equipment such as dust mask, eyeshields, and gloves. No significant toxicity has been reported at the concentrations used in research. Comprehensive toxicology studies are lacking. It is not an approved drug and is intended for research use only.
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| References |
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| Additional Infomation |
2-[2-(4-aminophenyl)-3H-benzimidazole-5-yl]-3H-benzimidazole-5-amine is a member of the benzimidazole class of compounds.
RO 90-7501 is a multifunctional research compound with activities including Aβ42 fibril assembly inhibition, TPR-dependent PP5 inhibition, ATM phosphorylation suppression, and selective enhancement of TLR3/RLR-mediated antiviral responses. It has significant radiosensitizing effects on cervical cancer cells and inhibits DNA damage response by inhibiting ATM. It is also known as a prototypic inhibitor for Aβ42 fibril formation. It is not approved for clinical use. |
| Molecular Formula |
C20H16N6
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|---|---|
| Molecular Weight |
340.39
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| Exact Mass |
340.144
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| CAS # |
293762-45-5
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| PubChem CID |
824226
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| Appearance |
Brown to breen solid powder
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| Density |
1.443g/cm3
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| Boiling Point |
751.035ºC at 760 mmHg
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| Flash Point |
449.122ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.842
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
493
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PAGZCEHLFCJSPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N6/c21-13-4-1-11(2-5-13)19-23-15-7-3-12(9-17(15)25-19)20-24-16-8-6-14(22)10-18(16)26-20/h1-10H,21-22H2,(H,23,25)(H,24,26)
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| Chemical Name |
2-[2-(4-aminophenyl)-3H-benzimidazol-5-yl]-3H-benzimidazol-5-amine
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| Synonyms |
RO 907501 RO 90 7501 RO 90-7501
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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 : ~41.67 mg/mL (~122.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.11 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9378 mL | 14.6890 mL | 29.3781 mL | |
| 5 mM | 0.5876 mL | 2.9378 mL | 5.8756 mL | |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9378 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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