RO5045337 MedChemExpress (MCE)

Product Name	RG7112
Synonyms	RG7112 RG 7112 CS-2164 p53 inhibitor RO5045337 (RG7112) p53 and MDM2 proteins-interaction-inhibitor [(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 RG 7112 CS-2164 p53 inhibitor RO5045337 (RG7112) p53 and MDM2 proteins-interaction-inhibitor [(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 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]-
CAS	939981-39-2
EINECS
Chemical Formula	C38H48Cl2N4O4S
Molecular Weight	727.78
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	RG7112 RG7112 MedChemExpress (MCE) HY-10959 939981-39-2 RO5045337 99.87% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions RG7112 RG7112 MedChemExpress (MCE) HY-10959 939981-39-2 RO5045337 99.87% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2. 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]. 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]. Kd: 11 nM (MDM2)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

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