1. Cell Cycle/DNA Damage MAPK/ERK Pathway GPCR/G Protein
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  3. KRAS-IN-54

KRAS-IN-54 is a macrocyclic KRAS inhibitor. KRAS-IN-54 exhibits activity against cell viability and pERK inhibition in cells with KRASG12D and KRASG13D mutations. KRAS-IN-54 can be used in the research of KRAS-mutant cancers, including pancreatic adenocarcinoma, colorectal cancer, non-small cell lung cancer, esophageal cancer, gallbladder cancer, melanoma, ovarian cancer and endometrial cancer.

For research use only. We do not sell to patients.

KRAS-IN-54

KRAS-IN-54 Chemical Structure

CAS No. : 3084918-70-4

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Description

KRAS-IN-54 is a macrocyclic KRAS inhibitor. KRAS-IN-54 exhibits activity against cell viability and pERK inhibition in cells with KRASG12D and KRASG13D mutations. KRAS-IN-54 can be used in the research of KRAS-mutant cancers, including pancreatic adenocarcinoma, colorectal cancer, non-small cell lung cancer, esophageal cancer, gallbladder cancer, melanoma, ovarian cancer and endometrial cancer[1].

IC50 & Target[1]

KRas G12D

 

KRAS G13D

 

In Vitro

KRAS-IN-54 (compound 3) inhibits the viability of AGS (KRASG12D) cells with an IC50 of 10 nM; it also inhibits the viability of HCT-116 (KRASG13D) cells with an IC50 of 27 nM[1].
KRAS-IN-54 inhibits ERK phosphorylation in AGS (KRASG12D) cells with an IC50 of 9 nM; it also inhibits ERK phosphorylation in HCT-116 (KRASG13D) cells with an IC50 of 10 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1192.39

Formula

C60H78F5N11O7S

CAS No.
SMILES

CO[C@H](C1=[C@@](C=C(C=N1)N2CCN(CC2)C)[C@@]3=C4CC(C)(COC([C@@H]5CCCN(C([C@H](CC6=NC(C7=CC4=C(N3CC(F)(F)F)C=C7F)=CS6)NC([C@@H](N(C(C8(F)CCN(C([C@H]9N(C)[C@@H]9C%10CC%10)=O)CC8)=O)C)C%11CCCC%11)=O)=O)N5)=O)C)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
KRAS-IN-54
Cat. No.:
HY-181704
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