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RG7112

Cat. No. M3628
RG7112 Structure
Synonym:

RO5045337

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 280 In stock
50mg USD 980 In stock
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Quality Control
Biological Activity

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice
Formulation 1% Klucel LF/0.1% Tween 80
Dosages 25–200 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 727.78
Formula C38H48Cl2N4O4S
CAS Number 939981-39-2
Purity 99.53%
Solubility DMSO
Storage at -20°C
References

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Vu B, et al. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. PMID: 24900694.

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Kevetrin hydrochloride

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

NSC 207895

NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

SL-01

SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RG7112, RO5045337 supplier, Mdm2, inhibitors

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