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LY-3537982

Chemical Structure : LY-3537982

CAS No.: 2414198-64-2

LY-3537982 (LY3537982)

Catalog No.: PC-72313Not For Human Use, Lab Use Only.

LY-3537982 (LY3537982) is a highly selective and potent KRAS-G12C inhibitor, selectively inhibits growth of KRAS G12C mutant cells (IC50=1-60 nM).

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Biological Activity

LY-3537982 (LY3537982) is a highly selective and potent KRAS-G12C inhibitor, selectively inhibits growth of KRAS G12C mutant cells (IC50=1-60 nM).
LY-3537982 does not inhibit growth of KRAS G12S/G13C/G12D mutant cells and WT KRAS cells (CI50>10 uM).
LY-3537982 displays high selectivity for proteome-wide cysteine residues was evaluated using competitive chemical proteomics (8866 peptides).
LY3537982 inhibits the growth of subcutaneous EL3187 NSCLC PDX tumors in nude mice in a dose dependent manner.
LY3537982 demonstrates robust tumor regression in combination with other agents in KRAS G12C in vivo models.
LY3537982 is a promising KRAS G12C inhibitor predicted to deliver >90% KRAS G12C target occupancy in the clinic.

Physicochemical Properties

M.Wt 500.905
Formula C23H15ClF2N4O3S
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

4-(2-acryloyl-9-chloro-7-fluoro-5-oxo-2,3,11,11a-tetrahydro-1H,5H-benzo[f]imidazo[5,1-c][1,4]oxazepin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile

References

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