[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone

Product Name: [(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone
CAS No.: 939981-39-2
Chemical Name: [(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone
Synonyms: RG7112;CS-2164;p53 inhibitor;RG7112;RG 7112;RG-7112 ，S7030;RG7112(RO5045337);RO5045337 (RG7112);RG7112, 10 mM in DMSO;RG-7112, MDM2 inhibitor;p53 and MDM2 proteins-interaction-inhibitor
CBNumber: CB62510101
Molecular Formula: C38H48Cl2N4O4S
Formula Weight: 727.78
MOL File: 939981-39-2.mol

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[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone Property

Density: 1.23
storage temp.: Store at -20°C
solubility: ≥36.4 mg/mL in DMSO; insoluble in H2O; ≥31.87 mg/mL in EtOH
form: solid
color: White to off-white
InChIKey: QBGKPEROWUKSBK-QPPIDDCLSA-N
SMILES: C(N1C(C2=CC=C(C(C)(C)C)C=C2OCC)=N[C@](C2=CC=C(Cl)C=C2)(C)[C@]1(C1=CC=C(Cl)C=C1)C)(N1CCN(CCCS(C)(=O)=O)CC1)=O

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML4102
Product name: RG7112
Purity: ≥98% (HPLC)
Packaging: 1 unit
Price: $319
Updated: 2025/07/31

Cayman Chemical

Product number: 25673
Product name: RG-7112
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 25673
Product name: RG-7112
Packaging: 25mg
Price: $887
Updated: 2024/03/01

Cayman Chemical

Product number: 25673
Product name: RG-7112
Packaging: 5mg
Price: $233
Updated: 2024/03/01

Cayman Chemical

Product number: 25673
Product name: RG-7112
Packaging: 10mg
Price: $437
Updated: 2024/03/01

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[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone Chemical Properties,Usage,Production

Description

RG-7112 is an inhibitor of mouse double-minute 2 protein (MDM2; IC₅₀ = 0.018 μM), an E3 ubiquitin ligase that ubiquitinates the tumor suppressor p53 and also acts as a negative regulator of p53 transcriptional activity. RG-7112 binds to the p53 binding pocket of MDM2. It increases the levels of p53 and its transcriptional targets in SJSA-1 osteosarcoma cells. It inhibits proliferation in cancer cell lines expressing wild-type p53 (IC₅₀s = 0.18-2.2 μM) and cell lines expressing mutant p53 (IC₅₀s = 5.7-20.3 μM). RG-7112 also prevents and reduces tumor growth in an SJSA-1 mouse xenograft model when administered at doses of 50 and 100 mg/kg per day, respectively. However, it inhibits thrombopoiesis in vivo, decreasing platelet counts in rats when administered at doses of 50 and 100 mg/kg and in cynomolgus monkeys at doses of 10 and 20 mg/kg.

Uses

RG 7112 is MDM2 antagonist. It can be used in biological study of single mouse analysis on evaluation of alternative in vivo drug screening methodology.

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].

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.

target

MDM2

References

[1] BINH VU*. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development[J]. ACS Medicinal Chemistry Letters, 2013, 4 5: 466-469. DOI: 10.1021/ml4000657
[2] CHRISTIAN TOVAR. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.[J]. Cancer research, 2013, 73 8: 2587-2597. DOI: 10.1158/0008-5472.can-12-2807
[3] CAMELIA IANCU-RUBIN . Activation of p53 by the MDM2 inhibitor RG7112 impairs thrombopoiesis[J]. Experimental hematology, 2014, 42 2: Pages 137-145.e5. DOI: 10.1016/j.exphem.2013.11.012

[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone Preparation Products And Raw materials

Raw materials

Preparation Products

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[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone Suppliers

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939981-39-2, [(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanoneRelated Search:

RG7112;RG 7112

CS-2164

[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone

p53 and MDM2 proteins-interaction-inhibitor

Methanone, [(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-diMethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-diMethyl-1H-iMidazol-1-yl][4-[3-(Methylsulfonyl)propyl]-1-piperazinyl]-

p53 inhibitor

RG7112

RO5045337 (RG7112)

RG7112(RO5045337)

[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone

(4S,5R)-2-[4-(tert-Butyl)-2-ethoxyphenyl]-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1-imidazolyl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone

RG-7112, MDM2 inhibitor

RG7112, 10 mM in DMSO

RG-7112 ，S7030

((4r,5s)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1h-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone

939981-39-2

C38H48Cl2N4O4S