Indacaterol maleate | ß2 adrenoceptor agonist/SRSF6 inhibitor

Indacaterol chemical structure

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Indacaterol maleate (753498-25-8) is a full agonist (pEC50 = 8.06) of the human ß2 adrenoceptor.1,2 Clinically important drug for the treatment of chronic obstructive pulmonary disease.  Indacaterol blocked colorectal cancer progression in vitro (IC50 = 19.01 µM) and in vivo via inhibition of the splicing factor SRSF6 by binding to its RRM2 domain.3 It also blocked cell migration in metastatic breast cancer MDA-MB-231 cells by a similar mechanism.4

References/Citations:

  1. Battram et al. (2006), In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled ß2 adrenoceptor agonist with a 24-h duration of action; J. Pharmacol. Exp. Ther. 317 762
  2. Sturton et al. (2008), Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist on small airways in human and rat precision-cut lung slices; J. Pharmacol. Exp. Ther. 324 270
  3. Wan et al. (2017), SRSF6-regulated alternative splicing that promotes tumour progression offers a therapy target for colorectal cancer; Gut 68 118
  4. Ayama-Canden et al. (2023), Indacaterol inhibits collective cell migration and IGDQ-mediated single cell migration in metastatic breast cancer MDA-MB-231 cells; Cell Commun. Signal. 21 301
753498-25-8, indacaterol, Indacaterol maleate supplier, Indacaterol supplier, Spliceosome inhibitor, SRSF6 inhibitor
Alternate Name:
QAB149

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Indacaterol maleate (753498-25-8) is a full agonist (pEC50 = 8.06) of the human ß2 adrenoceptor.1,2 Clinically important drug for the treatment of chronic obstructive pulmonary disease.  Indacaterol blocked colorectal cancer progression in vitro (IC50 = 19.01 µM) and in vivo via inhibition of the splicing factor SRSF6 by binding to its RRM2 domain.3 It also blocked cell migration in metastatic breast cancer MDA-MB-231 cells by a similar mechanism.4

References/Citations:

  1. Battram et al. (2006), In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled ß2 adrenoceptor agonist with a 24-h duration of action; J. Pharmacol. Exp. Ther. 317 762
  2. Sturton et al. (2008), Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist on small airways in human and rat precision-cut lung slices; J. Pharmacol. Exp. Ther. 324 270
  3. Wan et al. (2017), SRSF6-regulated alternative splicing that promotes tumour progression offers a therapy target for colorectal cancer; Gut 68 118
  4. Ayama-Canden et al. (2023), Indacaterol inhibits collective cell migration and IGDQ-mediated single cell migration in metastatic breast cancer MDA-MB-231 cells; Cell Commun. Signal. 21 301