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KO-947

Catalog No.GC33051

KO-947 es un inhibidor potente y selectivo de las quinasas ERK1/2 con utilidad potencial en tumores desregulados en la vÍa MAPK.

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KO-947 Chemical Structure

Cas No.: 1695533-89-1

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
203,00 $
Disponible
5mg
185,00 $
Disponible
10mg
255,00 $
Disponible
25mg
567,00 $
Disponible
50mg
681,00 $
Disponible
100mg
1.064,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical utility in MAPK pathway dysregulated tumors.

KO-947 is a 10 nM inhibitor of ERK with at least 50-fold selectivity against a panel of 450 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling, including mutations in BRAF, NRAS or KRAS, at low nanomolar concentrations[1].

In cell-line derived xenograft studies, KO-947 profoundly suppresses ERK signaling for up to five days after a single dose and induces regressions in RAS- and RAF-mutant melanoma, NSCLC and pancreatic cancer models on administration schedules ranging from daily to weekly. Intermittent dosing enables comparable antitumor activity at reduced dose-intensity[1].

[1]. Burrows F, et al. KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5168. doi:10.1158/1538-7445.AM2017-5168.

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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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