KRAS inhibitor 11( —— )

Catalog No. M16478 CAS No. 900897-56-5

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Datasheet

HNMR

HPLC

MSDS

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Product Name

KRAS inhibitor 11
Note

Research use only, not for human use.
Brief Description

KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor.
Description

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.
In Vitro

Western Blot Analysis Cell Line:BHK cells stably expressing KRASG12D Concentration:0.01, 0.1, 0.5 1, 5 μM Incubation Time:Result:Decreased the p-ERK levels at >1μM.
In Vivo

——
Synonyms

——
Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

Ras
Research Area

——
Indication

——

CAS Number

900897-56-5
Formula Weight

413.525
Molecular Formula

C25H27N5O
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (120.92 mM)
SMILES

CC1=NN2C(=CC(=NC2=C1C3=CC=CC=C3)C4=CC=CC=C4)N5CCN(CC5)CCO
Chemical Name

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

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

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