Selumetinib

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Product Code: 3256
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Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 1/2.

Chemical Name:
6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide

Biological Activity:
Biological Activity	Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 1/2.
Technical Data:
M.W.	457.68
Formula:	C<sub>17</sub>H<sub>15</sub>BrClFN<sub>4</sub>O<sub>3</sub>
Solubility:	DMSO
Purity:	98%
Storage:	-20℃
CAS No:	606143-52-6
References:
References	Huynh H, et al, Mol Cancer Therapy, 2007, 6 (1), 138-146 Garon EB, et al, Mol Cancer Thera, 2010, 9 (7), 1985-1994. Yeh TC, et al, Clin Cancer Res, 2007, 13 (5), 1576-1583. Huynh H, et al, Mol Cancer Ther, 2007, 6 (9), 2468-2476. Davies BR, et al. Mol Cancer Ther, 2007, 6(8), 2209-2219. Morelli MP, et al. Clin Cancer Res, 2012, 18(4), 1051-1062. Yuen JS, et al. Int J Oncol, 2012, 41(2), 712-720. Leboeuf R, et al. J Clin Endocrinol Metab, 2008, 93(6), 2194-2201. Emery CM,, et al. Proc Natl Acad Sci U S A, 2009, 106(48), 20411-20416. Friday BB, et al. Cancer Res, 2008, 68(15), 6145-6153. Huynh H, et al. J Hepatol, 2010, 52(1), 79-87. Diep CH, et al. Clin Cancer Res, 2011, 17(9), 2744-2756.

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