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LY-3214996

Chemical Structure : LY-3214996

CAS No.: 1951483-29-6

LY-3214996 (Temuterkib;LY3214996)

Catalog No.: PC-61973Not For Human Use, Lab Use Only.

Temuterkib (LY-3214996) is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Temuterkib (LY-3214996) is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays.
Temuterkib (LY-3214996) potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
Temuterkib (LY-3214996) demonstrates inhibition of cell proliferation, general sensitivitity against tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation.
Temuterkib (LY-3214996) significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models.

Physicochemical Properties

M.Wt 453.56
Formula C22H27N7O2S
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

4H-Thieno[2,3-c]pyrrol-4-one,5,6-dihydro-6,6-dimethyl-2-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-5-[2-(4-morpholinyl)ethyl]-

References

1. Shripad V. Bhagwat, et al. AACR Abstract 4973.

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