化合物RG7112 T6965
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 939981-39-2 | ¥6,680.00 | 询底价 |
10 mg | 939981-39-2 | ¥1,580.00 | 询底价 |
50 mg | 939981-39-2 | ¥4,680.00 | 询底价 |
5 mg | 939981-39-2 | ¥897.00 | 询底价 |
1 mg | 939981-39-2 | ¥398.00 | 询底价 |
1 mL | 939981-39-2 | ¥1,460.00 | 询底价 |
500 mg | 939981-39-2 | ¥13,500.00 | 询底价 |
2 mg | 939981-39-2 | ¥572.00 | 询底价 |
25 mg | 939981-39-2 | ¥3,160.00 | 询底价 |
Product Introduction
Bioactivity
英文名: RG7112
描述: RG7112 (RO5045337) 是一种口服生物可利用的选择性 p53-MDM2 抑制剂。
细胞实验: Cell lines: Three wild-type p53 (HCT116,RKO,and SJSA1) and 2 mutant p53 (SW480 and MDA-MB-435) cell lines. Concentrations: ~5 μM. Incubation Time: 5 d. Method: Cell proliferation/viability is evaluated by the tetrazolium dye (MTT) assay.Cell growth kinetics are measured using the IncuCyte live cell imaging system.For cell-cycle analysis,cells are cultured in T75 flask with appropriate growth medium (106 cells/condition in 10 mL) and incubated overnight at 37°C.They are incubated with test compounds and processed.
激酶实验: HTRF assay: Homogeneous time-resolved fluorescence (HTRF) assay measures the signal generated by 2 components when they are in close proximity. The p53–MDM2 binding assay uses a biotinylated peptide derived from the MDM2-binding domain of p53 and a truncated N-terminal portion of recombinant human GST-tagged MDM2 protein containing the p53-binding domain. Proteins for crystal structure studies are expressed in E. coli strain BL21 using the helper plasmid pUBS 520 coding for the lacIq repressor and the rare tRNAArg [AGA/AGG]. For crystallization, the frozen protein is thawed and concentrated to 9.8 mg/mL using a Centricon concentrator (3,000 MW cutoff). The complex is then formed by combining the protein with a slight molar excess of the inhibitor (stock solution is 100 mM in DMSO) and this solution is allowed to sit for 4 hours at 4°C. Cryopreserved crystals are used to collect diffraction data on beamline X8C at the National Synchrotron Light Source at Brookhaven National Laboratory.
动物实验: Animal Models: Nude mice bearing SJSA-1,MHMn,or LNCaP xenografts. Formulation: Suspended in 1% Klucel LF/0.1% Tween 80. Dosages: ~200 mg/kg. Administration: p.o.
体外活性: In three wild-type p53 (HCT116, RKO, and SJSA1) cell lines, RG7112 selectively and dose-dependently inhibits cell growth. In cancer cells expressing wild-type p53, RG7112 activates the p53 pathway, and induces cell-cycle arrest and apoptosis. RG7112, both alone and combined with Peg-IFNα 2a, significantly decreases MPN colony-forming unit-granulocyte macrophage and burst-forming unit-erythroid numbers and preferentially eliminates the total number of JAKV617F(+) MPN hematopoietic progenitor cells. In addition, in MDM2-amplified liposarcoma cells, RG7112 significantly synergizes with Trabectedin.
体内活性: In rats, RG7112 impairs thrombopoiesis via activation of p53. In the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 93 mg/mL (128 mM)
DMSO : 93 mg/mL (128 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字: E1 activating enzyme | Inhibitor | E1/E2/E3 Enzyme | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | E3 ligating enzyme | MDM-2/p53 | Ubiquitin ligase | RG7112 | E2 conjugating enzyme | RO 5045337 | inhibit | RO-5045337
相关产品: MG-277 | RITA | Ganoderic acid X | Tenovin-1 | RO8994 | AM-8735 | PhiKan 083 | p53-Mdm2 inhibitor 4 | Navtemadlin | Idasanutlin
相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library | Autophagy Compound Library | Stem Cell Differentiation Compound Library
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