Cat. No.: HY-10959

RG7112

(Synonyms: RO5045337)

23 Cited Publications

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Based on 23 publication(s) in Google Scholar

RG7112 is a potent, selective, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2.

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Pureté: 99.80%
CAS No.: 939981-39-2
Formule: C₃₈H₄₈Cl₂N₄O₄S
Masse moléculaire:727.78

Stockage:

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

RG7112 Chemical Structure

CAS No.: 939981-39-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (23)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

RG7112 is a potent, selective, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2^[1].

IC₅₀ & Target

Kd: 11 nM (MDM2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.5 μM Compound: 2g, RG7112	Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
MDA-MB-435	IC₅₀	9.9 μM Compound: 2g, RG7112	Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
RKO	IC₅₀	0.4 μM Compound: 2g, RG7112	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
SJSA-1	IC₅₀	0.3 μM Compound: 2g, RG7112	Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
SJSA-1	IC₅₀	581 nM Compound: RG7112	Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum	[PMID: 24456472]
SJSA-1	IC₅₀	581 nM Compound: RG7112	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum	[PMID: 24601644]
SW480	IC₅₀	16.6 μM Compound: 2g, RG7112	Cytotoxicity against human SW480 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay Cytotoxicity against human SW480 cells expressing p53 mutant assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]

In Vitro

RG7112 (0-5 μM) stabilizes wild-type p53 and induces p53 signaling in cancer cells. RG7112 effectively activates p53 functions in cancer cells^[1]^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

SJSA1 osteosarcoma cells.
Concentration:

0-5 μM.
Incubation Time:

0-60 hours.
Result:

Dose-dependently inhibited the growth and killed SJSA1 osteosarcoma cells expressing high levels of MDM2 protein due to MDM2 gene amplification.

Cell Cycle Analysis^[2]

Cell Line:

HCT116 and SJSA1 cells.
Concentration:

0-5 μM.
Incubation Time:

48 hours.
Result:

Induced a dose-dependent cell cycle block in G1 and G2/M phase and depletion of the S phase compartment.

In Vivo

RG7112 (25-200 mg/kg, single oral dose) activates p53 pathway and induces apoptosis in tumor cells in vivo^[2].
RG7112 (100 mg/kg, gavage once per day, 5 days/week for 3 weeks ) reduces tumor growth rate and increases survival in GBM models^[3].

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

Animal Model:

Female Balb/c nude mice^[2].
Dosage:

25-200 mg/kg.
Administration:

Orally, single dose.
Result:

At the highest dose level of RG7112 (200 mg/kg) only 1.2% (± 0.89 SD) of cells incorporated BrdU at 24 h post-dosing, vs. 14% (± 1.83 SD) of vehicle treated tumors.

Animal Model:

GBM cells were implanted into the brain of Athymic Nude mice (7 weeks old females, 10 animals/group)^[3].
Dosage:

100 mg/kg.
Administration:

Oral gavage, once per day, 5 days/week for 3 weeks.
Result:

Reduced tumor growth rate and increases survival in heterotopic and orthotopic animal models bearing MDM2-amplified GBM.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 939981-39-2
Appearance Solid
Masse moléculaire 727.78
Formule C₃₈H₄₈Cl₂N₄O₄S
Color White to off-white
SMILES

C[C@@]1([C@](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
Synonyms

RO5045337
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

Publications (23)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Adv Sci (Weinh)

SETD8C302R Mutation Revealed from Myofibroblastoma-Discordant Monozygotic Twins Leads to p53/p21 Deficit and WEE1 Inhibitor Sensitivity. [Abstract]

2020 Aug 5;7(19):2001041. PMID: 33042742
Nat Chem Biol

Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. [Abstract]

2018 Feb;14(2):118-125. PMID: 29200206
Clin Cancer Res

Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. [Abstract]

2016 Mar 1;22(5):1185-96. PMID: 26482041

RG7112 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2016 Mar 1;22(5):1185-96. [Abstract]

p53, p21 and MDM2 protein levels in MDM2-amplified GBM line treated with RG7112.
J Pharm Anal

Ursodeoxycholic acid inhibits the uptake of cystine through SLC7A11 and impairs de novo synthesis of glutathione. [Abstract]

2025 Jan;15(1):101068. PMID: 39902457
EMBO J

Residual apoptotic activity of a tumorigenic p53 mutant improves cancer therapy responses. [Abstract]

2019 Oct 15;38(20):e102096. PMID: 31483066
Apoptosis

Strong activation of p53 by actinomycin D and nutlin-3a overcomes the resistance of cancer cells to the pro-apoptotic activity of the FAS ligand. [Abstract]

2024 Oct;29(9-10):1515-1528. PMID: 39068622
Apoptosis

p53 m6A modulation sensitizes hepatocellular carcinoma to apatinib through apoptosis. [Abstract]

2022 Jun;27(5-6):426-440. PMID: 35503144
Mater Sci Eng C Mater Biol Appl

A stimuli-responsive combination therapy for recovering p53-inactivation associated drug resistance. [Abstract]

2020 Mar;108:110403. PMID: 31923941
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Clin Transl Med

Oncogenic driver and therapeutic target: Prolactin signalling axis in retroperitoneal sarcoma. [Abstract]

2026 May;16(5):e70669. PMID: 42083506
Clin Transl Med

USP7 inhibitors suppress tumour neoangiogenesis and promote synergy with immune checkpoint inhibitors by downregulating fibroblast VEGF. [Abstract]

2024 Apr;14(4):e1648. PMID: 38602256
Breast Cancer Res

First in class dual MDM2/MDMX inhibitor ALRN-6924 enhances antitumor efficacy of chemotherapy in TP53 wild-type hormone receptor-positive breast cancer models. [Abstract]

2021 Mar 4;23(1):29. PMID: 33663585
Cells

PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]

2026 Mar 5;15(5):473. PMID: 41827906
Int J Mol Sci

Improving Reporter Gene Assay Methodology for Evaluating the Ability of Compounds to Restore P53 Activity. [Abstract]

2022 Nov 10;23(22):13867. PMID: 36430341
Cancers (Basel)

Early-Stage Lung Adenocarcinoma MDM2 Genomic Amplification Predicts Clinical Outcome and Response to Targeted Therapy. [Abstract]

2022 Jan 29;14(3):708. PMID: 35158979
Gynecol Oncol

Anti-tumor activity of dual inhibition of phosphatidylinositol 3-kinase and MDM2 against clear cell ovarian carcinoma. [Abstract]

2019 Nov;155(2):331-339. PMID: 31493899
Biomedicines

The Strong Activation of p53 Tumor Suppressor Drives the Synthesis of the Enigmatic Isoform of DUSP13 Protein. [Abstract]

2024 Jun 28;12(7):1449. PMID: 39062022
Oncol Rep

Long non‑coding RNA PCAT6 promotes the development of osteosarcoma by increasing MDM2 expression. [Abstract]

2020 Dec;44(6):2465-2474. PMID: 33125146
Preprints

2023 Oct 25.
Preprints

2023 Sep 25, 2023091653.
Patent

US20230088286A1.
Oncotarget

MDM2 is a potential therapeutic target and prognostic factor for ovarian clear cell carcinomas with wild type TP53. [Abstract]

2016 Nov 15;7(46):75328-75338. PMID: 27659536

RG7112 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Nov 15;7(46):75328-75338. [Abstract]

Cell viability and activation of TP53 target proteins in clear cell carcinomas treated with RG7112. A and B. Time- (A) and dose-dependent (B) accumulation of MDM2, TP53, and TP21, as measured by western blotting. RG7112 is added at 2.5 μM in (A). C. Induction of TP53 phosphorylation and TP53 target proteins (TP21 and PUMA), as determined by western blotting. Cleaved PARP and survivin are also assessed to detect proapoptotic signaling.

Solvant et solubilité

In Vitro:

DMSO : 200 mg/mL (274.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.3740 mL

6.8702 mL

13.7404 mL

5 mM

0.2748 mL

1.3740 mL

2.7481 mL

10 mM

0.1374 mL

0.6870 mL

1.3740 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: ≥ 10 mg/mL (13.74 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.

Protocol 2

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

Solubility: ≥ 10 mg/mL (13.74 mM); Clear solution

This protocol yields a clear solution of ≥ 10 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 (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 5 mg/mL (6.87 mM); Clear solution

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.44 mM); Clear solution

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 (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Vu B, et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. [Content Brief]

[2]. Tovar C, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73(8):2587-97. [Content Brief]

[3]. Verreault M, et al. Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. Clin Cancer Res. 2016 Mar 1;22(5):1185-96. [Content Brief]

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	1.3740 mL	6.8702 mL	13.7404 mL	34.3510 mL
	5 mM	0.2748 mL	1.3740 mL	2.7481 mL	6.8702 mL
	10 mM	0.1374 mL	0.6870 mL	1.3740 mL	3.4351 mL
	15 mM	0.0916 mL	0.4580 mL	0.9160 mL	2.2901 mL
	20 mM	0.0687 mL	0.3435 mL	0.6870 mL	1.7176 mL
	25 mM	0.0550 mL	0.2748 mL	0.5496 mL	1.3740 mL
	30 mM	0.0458 mL	0.2290 mL	0.4580 mL	1.1450 mL
	40 mM	0.0344 mL	0.1718 mL	0.3435 mL	0.8588 mL
	50 mM	0.0275 mL	0.1374 mL	0.2748 mL	0.6870 mL
	60 mM	0.0229 mL	0.1145 mL	0.2290 mL	0.5725 mL
	80 mM	0.0172 mL	0.0859 mL	0.1718 mL	0.4294 mL
	100 mM	0.0137 mL	0.0687 mL	0.1374 mL	0.3435 mL

Keywords

RG7112

23 Cited Publications

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RG7112

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RG7112

Activité biologique

Chemical Information

Publications (23)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RG7112 Related Classifications

HY-10959 Related Classifications