- 商品介绍
- 规格参数
- 包装参数
General description
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 µM). 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 µM). Also diminishes the proliferation of Burkitt lymphoma cell lines expressing high levels of c-Myc (IC50 = 2.5 µM). 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 µM/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 µM in ATG-c-Myc-transformed cultures), while exhibiting much reduced or little potency against cultures transformed by v-Src (no inhibition up to 20 µM), v-Jun or PI 3-K H1047R (45.5% inhibition at 10 µM). Selectively inhibits Myc-dependent proliferation of human & avian cultures (Effective conc. 25 to 50 µM; IC50 1 to 10 µM), 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 µM. Reported to suppress MDA-MB-231-derived tumor expansion in mice (10 mg/kg/d i.p.) in vivo with 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 µM/plasma & 12.4 µM/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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Myc homodimer
Secondary Target
Myc-Max
Packaging
Packaged under inert gas
Preparation Note
Use only fresh DMSO for reconstitution.
Other Notes
Hart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA.111, 12556.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | brown |
| solubility | DMSO: 50 mg/mL |
| storage temp. | 2-8°C |
| SMILES string | [N+](=O)([O-])c1ccc(cc1)c2nc(cc(c2)c4ccc(cc4)C(=O)N)c3[o]ccc3 |
| InChI | 1S/C22H15N3O4/c23-22(26)16-5-3-14(4-6-16)17-12-19(15-7-9-18(10-8-15)25(27)28)24-20(13-17)21-2-1-11-29-21/h1-13H,(H2,23,26) |
| InChI key | GTTDVYCKFQYVNN-UHFFFAOYSA-N |
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| 重量(kg) |
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