MedChemExpress - Model RG7112 - 939981-39-2
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[1].MCE products for research use only. We do not sell to patients.
RG7112
MCE China：RG7112
Brand：MedChemExpress (MCE)
Cat. No.HY-10959
CAS：939981-39-2
Synonyms：RO5045337
Purity：99.87%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
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].
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].
IC50 & Target：Kd: 11 nM (MDM2)[1] Cellular Effect Cell Line Type Value Description References
Hot selling product：Clavulanic acid | (S)-Higenamine (hydrobromide) | ReACp53 | TASK-1-IN-1 | Oxiconazole nitrate | Hernandezine | Pafuramidine | RG7112 | Myristic acid | Aminopterin
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
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]
Brand introduction:
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