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KRAS G12C inhibitor 143D

Chemical Structure : KRAS G12C inhibitor 143D

CAS No.: 2820421-08-5

KRAS G12C inhibitor 143D (143D)

Catalog No.: PC-22872Not For Human Use, Lab Use Only.

143D is a highly potent and selective, BBB-permeable KRAS G12C inhibitor, inhibits the binding of KRASG12C and SOS1 with IC50 of 21.1 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

143D is a highly potent and selective, BBB-permeable KRAS G12C inhibitor, inhibits the binding of KRASG12C and SOS1 with IC50 of 21.1 nM.
143D shows little effect on the binding of KRASG12D and SOS1.
143D displays potent antiproliferative activity by causing cell cycle arrest and apoptosis, shows significant antiproliferative effects on the KRASG12C-transformed Ba/F3 cell line with IC50 of 10 nM.
143D selectively inhibits the constitutive activation of KRASG12C signaling pathways.
143D inhibits the KRAS signaling pathway and growth of KRASG12C-mutant tumors.

Physicochemical Properties

M.Wt 629.18
Formula C35H38ClFN6O2
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

(S)-2-(4-(7-(8-chloronaphthalen-1-yl)-2-((tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-5,6,7,8-tetrahydro-1,7-naphthyridin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile

References

1. Xu LS, et al. Acta Pharmacol Sin. 2023 Jul;44(7):1475-1486.

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