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Ro5-3335 (Ro-53335) is a novel, potent benzodiazepine-based inhibitor of core binding factor (CBF) with the potential for treating leukemia. As a RUNX1-CBFβ interaction inhibitor, it represses RUNX1/CBFB-dependent transactivation.
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| ln Vitro |
Ro5-3335 exhibits antiproliferative effect against human CBF leukemia cell lines, as demonstrated by its IC50 values of 1.1 μM, 21.7 μM, and 17.3 μM for ME-1, Kasumi-1, and REH, respectively[1]. In zebrafish embryos, Ro5-3335 prevents final hematopoiesis [1]. Although Ro5-3335 alters the complex's structure or widens the gap between RUNX1 and CBFβ, it does not entirely dissolve the RUNX1-CBFβ interaction[1].
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| ln Vivo |
In zebrafish models, Ro5-3335 has been found to be an inhibitor of RUNX1–CBFβ function[1]. ?A RUNX1-ETO transgenic zebrafish's preleukemic phenotype is salvaged by Ro5-3335[1]. ?In a mouse CBFB-MYH11 leukemia model, Ro5-3335 (300 mg/kg/d; po; for 30 days) lowers the burden of leukemia[1].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (leukemic model)[1]
Doses: 300 mg/kg Route of Administration: Oral administration; daily; for 30 days Experimental Results: decreased the number of c-kit+ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen. |
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| References | ||
| Additional Infomation |
Ro 5-3335 is a 1,4-benzodiazepinone that is nordazepam in which the phenyl substituent has been replaced by a 1H-pyrrol-2-yl group. It inhibits gene expression in HIV-1 at the transcriptional level through interference with Tat-mediated transactivation. It has a role as an antineoplastic agent, an anti-HIV-1 agent, a RUNX1 inhibitor and a HIV-1 Tat inhibitor. It is a 1,4-benzodiazepinone, an organochlorine compound and a member of pyrroles.
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| Molecular Formula |
C₁₃H₁₀CLN₃O
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|---|---|
| Molecular Weight |
259.691
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| Exact Mass |
259.051
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| CAS # |
30195-30-3
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| Related CAS # |
139339-45-0; 2328140-37-8 ;30195-30-3;
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| PubChem CID |
64983
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.46g/cm3
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| Boiling Point |
501.6ºC at 760mmHg
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| Melting Point |
256 °C (分解)
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| Flash Point |
257.1ºC
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| Index of Refraction |
1.712
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| LogP |
2.031
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XWNMORIHKRROGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10ClN3O/c14-8-3-4-10-9(6-8)13(11-2-1-5-15-11)16-7-12(18)17-10/h1-6,15H,7H2,(H,17,18)
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| Chemical Name |
7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one
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| Synonyms |
Ro5-3335 Ro 5 3335 CBFβ-Runx1 inhibitor II Ro 5-3335
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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 (~385.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.63 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 25.0 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: ≥ 2.5 mg/mL (9.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8507 mL | 19.2537 mL | 38.5075 mL | |
| 5 mM | 0.7701 mL | 3.8507 mL | 7.7015 mL | |
| 10 mM | 0.3851 mL | 1.9254 mL | 3.8507 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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