LY-3214996

Research use only, not for human use.

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

LY-3214996 is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays; potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines; demonstrates inhibition of cell proliferation, general sensitivitity against tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation; 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.Blood Cancer Phase 1 Clinical

LY 3214996;LY3214996

MAPK/ERK Signaling

ERK

ERK1;ERK2

Cancer

Blood cancer

1951483-29-6

453.56

C22H27N7O2S

>98% (HPLC)

DMSO: 12 mg/mL (26.5 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CC(N(CCN1CCOCC1)C2=O)(C)C3=C2C=C(S3)C4=CC=NC(NC5=CC=NN5C)=N4

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]-

(-20℃)

With Ice Pack

≥ 2 years