Size | Price | Stock | Qty |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Purity: ≥98%
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.
Targets |
MDM2 (Kd = 11 nM)
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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]
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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]
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Animal Protocol |
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References |
Molecular Formula |
C38H48CL2N4O4S
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Molecular Weight |
727.78
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Exact Mass |
726.28
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Elemental Analysis |
C, 62.71; H, 6.65; Cl, 9.74; N, 7.70; O, 8.79; S, 4.41
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CAS # |
939981-39-2
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Appearance |
White to off-white solid powder
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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
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InChi Key |
QBGKPEROWUKSBK-QPPIDDCLSA-N
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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
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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
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
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 |