Cat. No. Name Size Price Add Cart
KI1469GSK-26367715 mg$230
GSK-263677110 mg$330
GSK-263677150 mg$730
GSK-2636771100 mg$1130

Chemical Characteristic

Product NameGSK-2636771
CAS No.1372540-25-4
Molecular Weight 433.42
FormulaC22H19ClN6O2S
Chemical Name2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid
Smilesc1(nc2c(n1Cc1c(c(ccc1)C(F)(F)F)C)cc(cc2C(=O)O)N1CCOCC1)C
Chemical Structure

Biological activities

GSK-2636771 is a PI3K p110β isoform specific inhibitor. [1] GSK-2636771 inhibits PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 and 72 nM, respectively. [2] In PI3Kα, the reciprocal mutation changes GSK2636771 from inactive to an IC50 of 1.6 µM, at least a 60-fold change. [3]

References

[1] Weigelt B, et al. Genomic Determinants of PI3K Pathway Inhibitor Response in Cancer. Front Oncol. 2012, 2:109.
[2] Macauley D, et al. American Association for Cancer Research (AACR) - 103rd Annual Meeting. Drugs Fut, 2012, 37(6): 451.
[3] Zheng ZH, et al. Mechanisms of PI3Kβ-Selective Inhibition Revealed by Reciprocal Mutagenesis. ACS Chem. Biol., 2013, 8 (4): 679-683.

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