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RO 90-7501 (RO907501; RO-90-7501) is a novel and potent RLR (RIG-I-likereceptors) agonist with antiviral activity. Also acting as a promoter of IFN-β and an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
| 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].
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| 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].
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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. |
| References |
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| Additional Infomation |
2-[2-(4-aminophenyl)-3H-benzimidazol-5-yl]-3H-benzimidazol-5-amine is a member of benzimidazoles.
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| 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
|
| Heavy Atom Count |
26
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| Complexity |
493
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| Defined Atom Stereocenter Count |
0
|
| 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)
|
| 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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