半岛bd体育手机客户端 说明
一般描述
A cell-permeable, blood-brain barrier permeant, bioavailable trisubstituted pyridine compound that inhibits c-Myc transcriptional activity. Shown to directly bind to both the monomeric c-Myc (Kd= 6.5 nM) and to c-Myc-Max heterodimer (Kd= 13.4 nM) with high affinity and disrupt c-Myc-Max interaction. Displays a very weak affinity towards Max-Max homodimer (Kd>1 ?M). Also interferes with Max homodimerization, albeit to a lesser extent than c-Myc-Max heterodimerization. Shown to inhibit the c-Myc-driven proliferation of NCI-H460, MDA-MB-231, and SUM-159PT and several other cancer cell lines (IC50= 5-10 ?M). Also diminishes the proliferation of Burkitt lymphoma cell lines expressing high levels of c-Myc (IC50= 2.5 ?M). Suppresses the growth of MDA-MB-231 cells in a xenografted nude mice model (10 mg/kg, i.p., q.d.).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, trisubstituted pyridine compound that displays Myc-selective affinity (Kd= 6.5 nM/Myc homodimer, 13.4 nM/Myc-Max dimer, >1.0 ?M/Max homodimer) and is 4-times more potent against Myc-Max than Max-Max in DNA-binding assays. Effectively prevents focal microtumors formation following N-Myc, c-Myc, as well as ATG- or CAG-c-Myc transformation of cultured chick embryo fibroblasts/CEF (>99.9% inhibition at 10 ?M in ATG-c-Myc-transformed cultures), while exhibiting much reduced or little potency against cultures transformed by v-Src (no inhibition up to 20 ?M), v-Jun or PI 3-K H1047R (45.5% inhibition at 10 ?M). Selectively inhibits Myc-dependent proliferation of human & avian cultures (Effective conc. 25 to 50 ?M; IC501 to 10 ?M), while exhibiting little potency against Myc-independent growths of human skin fibroblasts, non-transformed, v-jun-transformed, or methylcholanthrene-transformed quail embryo fibroblasts even at a high concentration of 50 ?M. Reported to suppress MDA-MB-231-derived tumor expansion in mice (10 mg/kg/d i.p.)in vivowith a concomitant upregulation of N-Myc downregulated gene 1/NDRG1 protein level in tumor tissue. Pharmacokinetics studies reveal good blood-brain barrier permeability in mice ([Drug] = 3.5 ?M/plasma & 12.4 ?M/brain 4 h post single 10 mg/kg i.p. dosage) and a plasma half-life of 1.84 h in rats following a single i.v. dose of 1 mg/kg.
生化/生理作用
Cell permeable: yes
Secondary Target
Myc-Max
Primary Target
Myc homodimer
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Use only fresh DMSO for reconstitution.
其他说明
Hart, J.R., et al. 2014.Proc. Natl. Acad. Sci. USA.111,12556.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C22H15N3O4 |
| 分子量 | 385.37 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | brown |
| 溶解性 | DMSO: 50 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
