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REDX-05358

Chemical Structure : REDX-05358

CAS No.: 1884226-20-3

REDX-05358 (REDX 05358;REDX05358)

Catalog No.: PC-61974Not For Human Use, Lab Use Only.

REDX-05358 is a novel potent, highly selective, orally bioavailable pan RAF inhibitor with IC50 of 0.1, 0.68, 0.171, and 0.076 nM for ARAF, BRAF, BRAF (V600E), and CRAF, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

REDX-05358 is a novel potent, highly selective, orally bioavailable pan RAF inhibitor with IC50 of 0.1, 0.68, 0.171, and 0.076 nM for ARAF, BRAF, BRAF (V600E), and CRAF, respectively; denmonstrates high selectivity profile against a panel of 468 kinases, exhibits negligible paradoxical activation due to inhibition of both RAF monomers and dimers; not only inhibits MAPK signalling in BRAF V600E mutant tumor cells, but also in those harbouring NRAS and KRAS mutations; exhibits in vivo efficacy in BRAF V600E CRC xenograft model.

Physicochemical Properties

M.Wt 472.929
Formula C26H21ClN4O3
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

5-[[3-[5-(2-Chlorophenyl)-1H-imidazol-2-yl]chroman-6-yl]oxy]-3,4-dihydro-1H-1,8-naphthyridin-2-one

References

1. Helen Mason, et al. AACR, Abstract 5160.

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