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MRTX-849

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PERK (1) PROTACs (3) Ras (5) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (7)
Click Chemistry:	Alkynes (1)

6

Inhibitors & Agonists

1

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

Adagrasib 15+ Cited Publications MRTX849	Ras	Cancer
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .

MRTX849 acid	Ras	Cancer
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC₅₀s between 0.25 and 0.76 μM) .

MRTX849 ethoxypropanoic acid	Target Protein Ligand-Linker Conjugates Ras	Cancer
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC₅₀s between 0.25 and 0.76 μM) .

LC-2 epimer	PROTACs Ras	Cancer
LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849 .

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

LC-2 1 Publications Verification	PROTACs Ras	Cancer
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC₅₀s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .

Cat. No.	Product Name		Classification

HY-134654

MRTX849 analog 24

Alkynes

MRTX849 analog 24 is an alkyne-containing click probe analogue of KRAS G12C inhibitor MRTX849, which is used to research MRTX849 function .

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