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RG7112
SKU
HY-10959-10 mg
Category Reference compound
Tags Apoptosis;Metabolic Enzyme/Protease, Cancer, E1/E2/E3 Enzyme;MDM-2/p53
$120 – $950
Products Details
Product Description
– RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2[1].
Web ID
– HY-10959
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C38H48Cl2N4O4S
References
– [1]Vu B, et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9.|[2]Tovar C, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73(8):2587-97.|[3]Verreault M, et al. Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. Clin Cancer Res. 2016 Mar 1;22(5):1185-96.
CAS Number
– 939981-39-2
Molecular Weight
– 727.78
Compound Purity
– 99.91
SMILES
– C[C@@]1([C@](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 200 mg/mL (ultrasonic)
Target
– E1/E2/E3 Enzyme;MDM-2/p53
Pathway
– Apoptosis;Metabolic Enzyme/Protease
Product type
– Reference compound
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