2. Apoptosis Metabolic Enzyme/Protease
  3. MDM-2/p53 E1/E2/E3 Enzyme
  4. RO-5963

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.

For research use only. We do not sell to patients.

RO-5963 Chemical Structure

RO-5963 Chemical Structure

CAS No. : 1416663-77-8

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1 mg USD 220 In-stock
5 mg USD 700 In-stock
10 mg USD 1020 In-stock
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50 mg USD 2600 In-stock
100 mg USD 4000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

RO-5963 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].

IC50 & Target

IC50: ~17 nM (p53-MDM2), ~24 nM (p53-MDMX)[1]
In Vitro

RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines[1].
RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels[1].

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

RO-5963 Related Antibodies

Apoptosis Analysis[1]

Cell Line: ZR75-30, MCF7 cells
Concentration: 10, 20 μM
Incubation Time: 48 hours
Result: Potently showed apoptotic activity.

Western Blot Analysis[1]

Cell Line: LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 cells
Concentration: 10 μM
Incubation Time: 24 hour
Result: Effectively activated p53 and elevated p21 and MDM2 levels.
Molecular Weight

518.90

Formula

C24H21ClF2N4O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OCC(CO)NC(C(C1=CC(F)=C(F)C=C1)N2C(/C(NC2=O)=C\C(C3=CC=C4Cl)=CNC3=C4C)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (289.07 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 1.9272 mL 9.6358 mL 19.2715 mL
5 mM 0.3854 mL 1.9272 mL 3.8543 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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: ≥ 3.75 mg/mL (7.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.75 mg/mL (7.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9272 mL 9.6358 mL 19.2715 mL 48.1788 mL
5 mM 0.3854 mL 1.9272 mL 3.8543 mL 9.6358 mL
10 mM 0.1927 mL 0.9636 mL 1.9272 mL 4.8179 mL
15 mM 0.1285 mL 0.6424 mL 1.2848 mL 3.2119 mL
20 mM 0.0964 mL 0.4818 mL 0.9636 mL 2.4089 mL
25 mM 0.0771 mL 0.3854 mL 0.7709 mL 1.9272 mL
30 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6060 mL
40 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2045 mL
50 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9636 mL
60 mM 0.0321 mL 0.1606 mL 0.3212 mL 0.8030 mL
80 mM 0.0241 mL 0.1204 mL 0.2409 mL 0.6022 mL
100 mM 0.0193 mL 0.0964 mL 0.1927 mL 0.4818 mL
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RO-5963 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:

RO-59631416663-77-8RO5963RO 5963MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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