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LUT014

Chemical Structure : LUT014

CAS No.: 2274819-46-2

LUT014 (Omzirafenib, LUT-014)

Catalog No.: PC-27489Not For Human Use, Lab Use Only.

Omzirafenib (LUT014, LUT-014) is a potent and specific, topical BRAF kinase inhibitor with IC50 of 13.3 nM and 11.7 nM for BRAF-V600E and WT BRAF respectively, paradoxically activates mitogen-activated protein kinase (MAPK).

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Biological Activity

Omzirafenib (LUT014, LUT-014) is a potent and specific, topical BRAF kinase inhibitor with IC50 of 13.3 nM and 11.7 nM for BRAF-V600E and WT BRAF respectively, paradoxically activates mitogen-activated protein kinase (MAPK).
LUT014 shows clear selectivity in vitro kinase inhibition profiling study against 59 human recombinant kinases.
inhibits proliferation of the KRASG12C-mutated human pancreatic cancer cell line MIA-PaCa-2.
LUT014 overrides the MAPK pathway inhibition, resulting in an increase in phosphorylated ERK1/2 (pERK) signaling in skin cells.
LUT014 could improve skin toxicities induced by EGFR inhibitors.

Physicochemical Properties

M.Wt 528.50
Formula C27H19F3N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N5-(3-(7H-Purin-6-yl)pyridin-2-yl)-6-methyl-N1-(3-(trifluoromethoxy)phenyl)isoquinoline-1,5-diamine

References

1. Lacouture ME, et al. Cancer Discov. 2021 Sep;11(9):2158-2167.

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