RG7112
RG7112
CAS: 939981-39-2
Molecular Formula: C38H48Cl2N4O4S
RG7112 - Names and Identifiers
RG7112 - Physico-chemical Properties
| Molecular Formula | C38H48Cl2N4O4S |
| Molar Mass | 727.78 |
| Density | 1.23 |
| Storage Condition | -20℃ |
| In vitro study | RG7112 is a potent and selective MDM2 antagonist, a member of the Nutlin family, and is currently in Phase I clinical studies. RG7112 binds MDM2 with high affinity (K D of 10.7 nM), blocking its interaction with p53 in vitro. The crystal structure of the RG7112-MDM2 complex indicates that the small molecule binds to the p53 pocket of MDM2, mimicking the interaction of important p53 amino acid residues. Treatment of cancer cells expressing wild-type p53 by RG7112 activates the p53 pathway, leading to cell cycle arrest and apoptosis. RG7112 exhibited potent anti-tumor activity against a panel of tumor cell lines. However, their anti-apoptotic activity was quite different, with optimal responses observed in MDM2 gene-amplified osteosarcoma cells. |
| In vivo study | RG7112 activates the p53 pathway in vivo and induces tumor cell apoptosis. Oral administration of RG7112 to human xenograft-bearing mice at nontoxic concentrations caused dose-dependent changes in proliferation/apoptosis biomarkers, as well as tumor suppression and regression. Notably, RG7112 was highly synergistic with chemical castration in LNCaP xenograft tumors. |
RG7112 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.374 ml | 6.87 ml | 13.74 ml |
| 5 mM | 0.275 ml | 1.374 ml | 2.748 ml |
| 10 mM | 0.137 ml | 0.687 ml | 1.374 ml |
| 5 mM | 0.027 ml | 0.137 ml | 0.275 ml |
Last Update：2024-01-02 23:10:35
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Mobile: +86-18621343501
QQ: 2881950922
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Product Name: RO5045337 Visit Supplier Webpage Request for quotationCAS: 939981-39-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
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Mobile: 609-228-6898
Product Name: RG7112 Visit Supplier Webpage Request for quotation
CAS: 939981-39-2
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 939981-39-2
Tel: 18301782025
Email: 3008007409@qq.com
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