RG7112

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

p53-MDM2 相互作用的有效选择性抑制剂；以高亲和力 (Kd=11 nM) 结合 MDM2。

A potent and selective inhibitor of p53-MDM2 interaction; binds MDM2 with high affinity (Kd=11 nM); stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. orally bioactive.(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.(In Vivo):RG7112 (25-200 mg/kg, single oral dose) activates p53 pathway and induces apoptosis in tumor cells in vivo.RG7112 (100 mg/kg, gavage once per day, 5 days/week for 3 weeks ) reduces tumor growth rate and increases survival in GBM models.

Cell Proliferation Assay 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 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.

Animal Model:Female Balb/c nude mice.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).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.

RG-7112 | RG 7112

Apoptosis

MDM2-p53

Mdm2

Cancer

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939981-39-2

727.7831

C38H48Cl2N4O4S

>98% (HPLC)

10 mM in DMSO

CCOC1=C(C=CC(=C1)C(C)(C)C)C2=NC(C(N2C(=O)N3CCN(CC3)CCCS(=O)(=O)C)(C)C4=CC=C(C=C4)Cl)(C)C5=CC=C(C=C5)Cl

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]-

(-20℃)

With Ice Pack

≥ 2 years