RG-7112 (RO-5045337)

Alias: RG7112; RG-7112; RG 7112; RO5045337; RO 5045337; RO5045337
Cat No.:V0045 Purity: ≥98%
RG7112(also known as RO5045337) is a novel, potent and highly selective antagonist/inhibitor of thep53-MDM2 protein-protein interaction withIC50of 11 nM.
RG-7112 (RO-5045337) Chemical Structure CAS No.: 939981-39-2
Product category: Mdm2
This product is for research use only, not for human use. We do not sell to patients.
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5mg
10mg
25mg
50mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

RG7112 (also known as RO5045337) is a novel, potent and highly selective antagonist/inhibitor of the p53-MDM2 protein-protein interaction with IC50 of 11 nM. For the treatment of cancer, RG-7112 is currently undergoing clinical testing.

Biological Activity I Assay Protocols (From Reference)
Targets
MDM2 (Kd = 11 nM)
ln Vitro
RG7112 is a potent and selective member of the nutlin family of MDM2 antagonists currently in phase I clinical studies. In vitro, MDM2's interactions with p53 are blocked by RG7112's highly specific binding of MDM2 (KD of 10.7 nM). The RG7112-MDM2 complex has been crystallized, and it shows that the small molecule mimics the interactions of crucial p53 amino acid residues by binding to MDM2's p53 pocket. By activating the p53 pathway, RG7112 causes cell-cycle arrest and apoptosis in cancer cells that express wild-type p53. A panel of solid tumor cell lines is sensitive to the antitumor effects of RG7112. However, the apoptotic activity of this drug varies greatly, with osteosarcoma cells that have MDM2 gene amplification showing the best response. [1]
ln Vivo
In vivo, RG7112 causes tumor cells to undergo apoptosis and activates the p53 pathway. At nontoxic doses, oral administration of RG7112 to mice bearing human xenografts resulted in dose-dependent alterations in proliferation/apoptosis biomarkers as well as tumor inhibition and regression. Notably, androgen deprivation and RG7112 have powerful synergistic effects in LNCaP xenograft tumors. [1]
Animal Protocol
1% Klucel LF/0.1% Tween 80; 200 mg/kg; oral taken
SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice
References
[1]. ACS Med Chem Lett . 2013 Apr 2;4(5):466-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C38H48CL2N4O4S
Molecular Weight
727.78
Exact Mass
726.28
Elemental Analysis
C, 62.71; H, 6.65; Cl, 9.74; N, 7.70; O, 8.79; S, 4.41
CAS #
939981-39-2
Appearance
White to off-white solid powder
SMILES
CCOC1=C(C=CC(=C1)C(C)(C)C)C2=N[C@@]([C@@](N2C(=O)N3CCN(CC3)CCCS(=O)(=O)C)(C)C4=CC=C(C=C4)Cl)(C)C5=CC=C(C=C5)Cl
InChi Key
QBGKPEROWUKSBK-QPPIDDCLSA-N
InChi Code
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
Chemical Name
[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
Synonyms
RG7112; RG-7112; RG 7112; RO5045337; RO 5045337; RO5045337
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~137.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: N/A
Solubility (In Vivo)
1%CMC Na: 14mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.3740 mL 6.8702 mL 13.7404 mL
5 mM 0.2748 mL 1.3740 mL 2.7481 mL
10 mM 0.1374 mL 0.6870 mL 1.3740 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00623870 Completed Drug: RO5045337 Hematologic Neoplasms Hoffmann-La Roche May 2008 Phase 1
NCT00559533 Completed Drug: RO5045337 Neoplasms Hoffmann-La Roche December 2007 Phase 1
Biological Data
  • RG-7112

  • RG-7112


  • RG-7112


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