Network Version
Selumetinib Data Sheet
| Product Name: | Selumetinib |
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| CAS No.: | 606143-52-6 | |
| Cat. No.: | HY-50706 | |
| MWt: | 457.68 | |
| Formula: | C17H15BrClFN4O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : 10 mg/mL (21.85 mM; Need ultrasonic); H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
IC50 & Target: IC50: 12 nM (MEK)[4], 14 nM (MEK1)[3]
In Vitro: Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells[1]. Selumetinib (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells[2]. Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line[3]. In Vivo: Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts[1]. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model[3]. |
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