KRASG12C IN-15

KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRASG12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRASG12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models[1].

Product Specifications

CAS Number

[2768868-14-8]

UNSPSC

12352005

Target

ERK; Ras

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; Stem Cell/Wnt

Field of Research

Cancer

Smiles

FC1=C(N2CC3(CN(C(C=C)=O)C3)CC2)N=C([C@H](C4)C(C)(C)[C@H]4C5)C5=C1C6=CC(O)=CC7=C6C=CC=C7

Molecular Formula

C31H32FN3O2

Molecular Weight

497.60

References & Citations

[1]Huang D, et al., Identification of Structurally Novel KRASG12C Inhibitors through Covalent DNA-Encoded Library Screening. J Med Chem. 2025 Feb 27;68 (4) :4801-4817.