RG7112

SKU: orb1300306

Description

RG7112

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 939981-39-2
• MW: 727.78
• Purity: 99.90%
• Formula: C₃₈H₄₈Cl₂N₄O₄S
• SMILES: CCOc1cc(ccc1C1=NC(C)(c2ccc(Cl)cc2)C(C)(N1C(=O)N1CCN(CCCS(C)(=O)=O)CC1)c1ccc(Cl)cc1)C(C)(C)C
• Target: MDM-2/p53,E1/E2/E3 Enzyme,Mdm2
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (127.79 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:10 mg/mL (13.74 mM);Ethanol:93 mg/mL (127.79 mM)

Bioactivity

• Target IC50:
  MDM2:11 nM(Kd)
• In Vivo:
  In rats, RG7112 impairs thrombopoiesis via activation of p53. in the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression.
• In Vitro:
  In three wild-type p53 (HCT116, RKO, and SJSA1) cell lines, RG7112 selectively and dose-dependently inhibits cell growth. In cancer cells expressing wild-type p53, RG7112 activate the p53 pathway, and induces cell-cycle arrest and apoptosis. RG7112, both alone and combined with Peg-IFNα 2a, significantly decreases MPN colony-forming unit-granulocyte macrophage and burst-forming unit-erythroid numbers and preferentially eliminate the total number of JAKV617F(+) MPN hematopoietic progenitor cells. In addition, in MDM2-amplified liposarcoma cells, RG7112 significantly synergizes with Trabectedin.
• Cell Research:
  Cell lines: Three wild-type p53 (HCT116,RKO and SJSA1) and 2 mutant p53 (SW480 and MDA-MB-435) cell lines. concentration : ~5 μM. Incubation Time: 5 d. Method: Cell proliferation/viability is evaluated b the tetrazolium dye (MTT) assay.Cell growth kinetics are measured usin the IncuCyte live cell imaging system.For cell-cycle analysis,cells are cultured in T75 flask with appropriate growth medium (106 cells/condition in 10 mL) and incubated overnight at 37℃.They are incubated with test compounds and processed.
• Animal Research:
  Animal Models: Nude mice bearing SJSA-1,MHMn,or LNCaP xenografts. Formulation: Suspended in 1% Klucel LF/0.1% Tween 80. Dosages: ~200 mg/kg. Administration: p.o.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Mdm2, MDM-2/p53, E3 ligating enzyme, E1 Enzyme, E1/E2/E3 Enzyme, E2 conjugating enzyme, E1Enzyme, E2 Enzyme, E2Enzyme, E3 Enzyme, E3Enzyme, E1 activating enzyme, RG7112, RG-7112, RG 7112, RO 5045337, RO5045337, RO-5045337, Ubiquitin ligase, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme

Compound Identifiers

PubChem CID

76525291