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  4. Ro5-3335

Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.

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Ro5-3335 Chemical Structure

Ro5-3335 Chemical Structure

CAS No. : 30195-30-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Ro5-3335 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation[1].

IC50 & Target

RUNX1-CBFβ interaction[1]
Cellular Effect
Cell Line Type Value Description References
SW480 IC50
4 μM
Compound: 1
The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay
The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay
[PMID: 7650672]
In Vitro

Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively[1].
? Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos[1].
? Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ro5-3335 Related Antibodies
In Vivo

Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models[1].
Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish[1].
Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (leukemic model)[1]
Dosage: 300 mg/kg
Administration: Oral administration; daily; for 30 days
Result: Reduced the number of c-kit+ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen.
Molecular Weight

259.69

Formula

C13H10ClN3O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CN3)=NC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (385.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.52%

SDS (393 KB)

COA (258 KB) HNMR (273 KB) RP-HPLC (256 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8507 mL 19.2537 mL 38.5075 mL 96.2686 mL
5 mM 0.7701 mL 3.8507 mL 7.7015 mL 19.2537 mL
10 mM 0.3851 mL 1.9254 mL 3.8507 mL 9.6269 mL
15 mM 0.2567 mL 1.2836 mL 2.5672 mL 6.4179 mL
20 mM 0.1925 mL 0.9627 mL 1.9254 mL 4.8134 mL
25 mM 0.1540 mL 0.7701 mL 1.5403 mL 3.8507 mL
30 mM 0.1284 mL 0.6418 mL 1.2836 mL 3.2090 mL
40 mM 0.0963 mL 0.4813 mL 0.9627 mL 2.4067 mL
50 mM 0.0770 mL 0.3851 mL 0.7701 mL 1.9254 mL
60 mM 0.0642 mL 0.3209 mL 0.6418 mL 1.6045 mL
80 mM 0.0481 mL 0.2407 mL 0.4813 mL 1.2034 mL
100 mM 0.0385 mL 0.1925 mL 0.3851 mL 0.9627 mL
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Ro5-3335 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ro5-333530195-30-3OtherscorebindingfactorCBFleukemiaRUNX1CBFβRUNX1-CBFBinteractionInhibitorinhibitorinhibit

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