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KRAS inhibitor 11

Chemical Structure : KRAS inhibitor 11

CAS No.: 900897-56-5

KRAS inhibitor 11

Catalog No.: PC-36140Not For Human Use, Lab Use Only.

KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway.

Physicochemical Properties

M.Wt 413.525
Formula C25H27N5O
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

2-[4-(8-methyl-3,9-diphenyl-2,6,7-triazabicyclo[4.3.0]nona-2,4,7,9-tetraen-5-yl)piperazin-1-yl]ethanol

References

1. McCarthy MJ, et al. ACS Omega. 2019 Feb 28;4(2):2921-2930.

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