SMILES string
[S](=O)(=O)(CCCN1CCN(CC1)C(=O)N2[C@]([C@](N=C2c5c(cc(cc5)C(C)(C)C)OCC)(C)c4ccc(cc4)Cl)(C)c3ccc(cc3)Cl)C
InChI
1S/C38H48Cl2N4O4S/c1-8-48-33-26-29(36(2,3)4)14-19-32(33)34-41-37(5,27-10-15-30(39)16-11-27)38(6,28-12-17-31(40)18-13-28)44(34)35(45)43-23-21-42(22-24-43)20-9-25-49(7,46)47/h10-19,26H,8-9,20-25H2,1-7H3/t37-,38+/m0/s1
InChI key
QBGKPEROWUKSBK-QPPIDDCLSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active, potent and selective MDM2 inhibitor with anti-cancer efficacy in cultures and in vivo by induces p53-dependent cell cycle arrest and apoptosis.
RG7112 is an orally active, potent and selective MDM2 inhibitor that binds and blocks p53-binding site (IC50 = 18 nM), thereby induces p53-dependent cell cycle arrest and apoptosis (av GI50 by MTT assays = 0.4 μM/wt 53 vs 33.4 μM/mutant p53) by stabilizing cellular p53. When administered in vivo, RG7112 is efficacious against the growth of tumor xenografts in mice (SJSA-1, SJSA-1luc2, and MHM; 25-200 mg/kg via daily p.o.).
RG7112 is an orally active, potent and selective MDM2 inhibitor that binds and blocks p53-binding site (IC50 = 18 nM), thereby induces p53-dependent cell cycle arrest and apoptosis (av GI50 by MTT assays = 0.4 μM/wt 53 vs 33.4 μM/mutant p53) by stabilizing cellular p53. When administered in vivo, RG7112 is efficacious against the growth of tumor xenografts in mice (SJSA-1, SJSA-1luc2, and MHM; 25-200 mg/kg via daily p.o.).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Binh Vu et al.
ACS medicinal chemistry letters, 4(5), 466-469 (2014-06-06)
The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its negative regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity.
Christian Tovar et al.
Cancer research, 73(8), 2587-2597 (2013-02-13)
MDM2 negatively regulates p53 stability and many human tumors overproduce MDM2 as a mechanism to restrict p53 function. Thus, inhibitors of p53-MDM2 binding that can reactivate p53 in cancer cells may offer an effective approach for cancer therapy. RG7112 is
Brian Higgins et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 20(14), 3742-3752 (2014-05-09)
Antitumor clinical activity has been demonstrated for the MDM2 antagonist RG7112, but patient tolerability for the necessary daily dosing was poor. Here, utilizing RG7388, a second-generation nutlin with superior selectivity and potency, we determine the feasibility of intermittent dosing to
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