Cat. No.: HY-16999

RO8994

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RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC₅₀ value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model.

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Pureté: 99.70%
CAS No.: 1309684-94-3
Formule: C₃₁H₃₁Cl₂FN₄O₄
Masse moléculaire:613.51

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RO8994 Chemical Structure

CAS No.: 1309684-94-3

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
SJSA-1	IC₅₀	0.013 μM Compound: RO8994	Antiproliferative activity against human SJSA cells expressing wild-type p53 by MTT assay Antiproliferative activity against human SJSA cells expressing wild-type p53 by MTT assay	[PMID: 24900784]
SW480	IC₅₀	5.19 μM Compound: RO8994	Antiproliferative activity against human SW480 cells expressing p53 mutant by MTT assay Antiproliferative activity against human SW480 cells expressing p53 mutant by MTT assay	[PMID: 24900784]

In Vitro

RO8994 dose-dependently and non-genotoxically induces p53 stabilization, cell cycle arrest and Apoptosis in tumor cells retainingwt p53^[3].

Activity Results for RO8994 in a Biochemical Binding Assay and Human Cancer Cell Proliferation Assays^[1]^[2]^[3]<

compd	HTRF IC₅₀ (nM)	SJSA IC₅₀ (μM)	SW480 IC₅₀ (μM)
RO8994	5	0.013	5.19

Antiproliferative Activity of RO8994 in Human Cancer Cell lines^[1]^[2]^[3]<

compd	MTT IC₅₀ (μM)	selectivity
RO8994	0.02	312

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

In Vivo

RO8994 inhibits tumor growth in human SJSA1 tumor xenografts models^[3].

Human Liver Microsomal Stability and Mean Single Dose PK Parameters of RO8994 in C57 Male Mice by Oral and IV Dosing^[1]^[2]^[3]<

compd	HLM_{_}CL (mL/min/kg)	PO dose (mg/kg)	PO AUC/dose (μg·hr/mL/mg/kg)	PO C_max (μg/mL)	IV dose (mg/kg)	CL (mL/min/kg)	t_1/2 (h)	F (%)
RO8994	7.5	25	3.7	5.8	0.64	5.8	7.1	92

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

Chemical Information

CAS No. 1309684-94-3
Appearance Solid
Masse moléculaire 613.51
Formule C₃₁H₃₁Cl₂FN₄O₄
Color White to off-white
SMILES

O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)NC5=CC=C(C(N)=O)C=C5OC
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : ≥ 45 mg/mL (73.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6300 mL

8.1498 mL

16.2997 mL

5 mM

0.3260 mL

1.6300 mL

3.2599 mL

10 mM

0.1630 mL

0.8150 mL

1.6300 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (3.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (3.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang Z, et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22(15):4001-4009. [Content Brief]

[2]. Zhang Z, et al. Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development. ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. [Content Brief]

[3]. Yu B, Liu H M. The development of new spirooxindoles targeting the p53–MDM2 protein-protein interactions for cancer therapy[J]. Targeting Protein-Protein Interactions by Small Molecules, 2018: 213-237.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.6300 mL	8.1498 mL	16.2997 mL	40.7491 mL
	5 mM	0.3260 mL	1.6300 mL	3.2599 mL	8.1498 mL
	10 mM	0.1630 mL	0.8150 mL	1.6300 mL	4.0749 mL
	15 mM	0.1087 mL	0.5433 mL	1.0866 mL	2.7166 mL
	20 mM	0.0815 mL	0.4075 mL	0.8150 mL	2.0375 mL
	25 mM	0.0652 mL	0.3260 mL	0.6520 mL	1.6300 mL
	30 mM	0.0543 mL	0.2717 mL	0.5433 mL	1.3583 mL
	40 mM	0.0407 mL	0.2037 mL	0.4075 mL	1.0187 mL
	50 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8150 mL
	60 mM	0.0272 mL	0.1358 mL	0.2717 mL	0.6792 mL

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RO8994

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

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Anti-Aging Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RO8994 Related Classifications

HY-16999 Related Classifications