K-Ras(G12C) inhibitor 6

K-Ras(G12C) inhibitor 6
Names
	Preferred IUPAC name N-{1-[(2,4-Dichlorophenoxy)acetyl]piperidin-4-yl}-4-sulfanylbutanamide
Identifiers
CAS Number	2060530-16-5;
3D model (JSmol)	Interactive image;
ChemSpider	31042597;
PubChem CID	71815954;
UNII	JPV55C3PN4 ;
	InChI InChI=1S/C17H22Cl2N2O3S/c18-12-3-4-15(14(19)10-12)24-11-17(23)21-7-5-13(6-8-21)20-16(22)2-1-9-25/h3-4,10,13,25H,1-2,5-9,11H2,(H,20,22) Key: ZPXCEHMKUTXHRZ-UHFFFAOYSA-N;
	SMILES SCCCC(=O)NC1CCN(CC1)C(=O)COC1=CC=C(Cl)C=C1Cl;
Properties
Chemical formula	C17H22Cl2N2O3S
Molar mass	405.33 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

K-Ras(G12C) inhibitor 6 is an inhibitor of the oncogene KRAS.

Its family of inhibitors allosterically control the GTP affinity of mutant K-Ras which is a driver in many cancers.

In recent years, significant research efforts have focused on finding effective inhibitors for the Kras-G12C mutation leading to the FDA-approval of G12C-KRAS targeting therapies including sotorasib (Lumakras) ^[1] and Adagrasib (MRTX849)^[2]

K-Ras(G12C) inhibitor 6 is an irreversible inhibitor subverting the native nucleotide preference to favour GDP over GTP.

References

^ "Sotorasib is First KRAS Inhibitor Approved by FDA - NCI". www.cancer.gov. 2021-06-25. Retrieved 2023-12-09.
^ Dhillon, Sohita (February 2023). "Adagrasib: First Approval". Drugs. 83 (3): 275–285. doi:10.1007/s40265-023-01839-y. ISSN 1179-1950. PMID 36763320.

[1] "Sotorasib is First KRAS Inhibitor Approved by FDA - NCI". www.cancer.gov. 2021-06-25. Retrieved 2023-12-09.

[2] Dhillon, Sohita (February 2023). "Adagrasib: First Approval". Drugs. 83 (3): 275–285. doi:10.1007/s40265-023-01839-y. ISSN 1179-1950. PMID 36763320.

[1]

[2]