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Rociletinib hydrobromide (CO-1686 (hydrobromide))

Catalog No.GC33061

El bromhidrato de rociletinib (CO-1686 (bromhidrato)) (bromhidrato de CO-1686) es un inhibidor de la cinasa administrado por vÍa oral que se dirige especÍficamente a las formas mutantes de EGFR, incluido T790M, y los valores de Ki para EGFRL858R/T790M y EGFRWT son 21,5 nM y 303,3 nM, respectivamente.

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Rociletinib hydrobromide (CO-1686 (hydrobromide)) Chemical Structure

Cas No.: 1446700-26-0

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
63,00 $
Disponible
5mg
45,00 $
Disponible
10mg
72,00 $
Disponible
50mg
135,00 $
Disponible
100mg
225,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition[1].

Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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