KO-947

Research use only, not for human use.

KO-947 is a potent and selective inhibitor of ERK1/2 kinase in biochemical, cellular and in vivo antitumor activity assays.

KO-947 is a potent and selective inhibitor of ERK1/2 kinase in biochemical, cellular and in vivo antitumor activity assays; 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.Solid Tumors Phase 1 Clinical(In Vitro):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.(In Vivo):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.

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.

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.

KO 947 | KO947

MAPK/ERK Signaling

ERK

ERK

Cancer

Solid Tumors

1695533-89-1

355.401

C21H17N5O

>98% (HPLC)

DMSO : 62.5 mg/mL 175.86 mM

O=C1NC2=CC(NN=C3C4=CC=NC=C4)=C3C=C2CN1CC5=CC=CC=C5

6-benzyl-3-(pyridin-4-yl)-1,5,6,8-tetrahydro-7H-pyrazolo[4,3-g]quinazolin-7-one

(-20℃)

With Ice Pack

≥ 2 years