Search Result

Results for "

mrtx

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Caspase (1) CDK (1) Drug Intermediate (1) Fluorescent Dye (1) Histone Methyltransferase (5) Isotope-Labeled Compounds (1) NADPH Oxidase (1) PARP (1) PERK (1) PROTACs (3) Ras (13) SOS1 (1) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (22) Neurological Disease (1)
Click Chemistry:	Alkynes (5)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134813

MRTX1133 45+ Cited Publications	Ras	Cancer
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

HY-130149

Adagrasib Maximum Cited Publications 57 Publications Verification 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 .

HY-139611

Navlimetostat 3 Publications Verification mrtx-1719; BMS-986504	Histone Methyltransferase	Cancer
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC₅₀ of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .

HY-137516

LC-2 2 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 .

HY-145926

MRTX0902 2 Publications Verification	SOS1 Ras	Neurological Disease Cancer
MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a K_i of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .

HY-114436

MRTX-1257 5 Publications Verification	Ras	Cancer
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-W095670

2,4,7-Trichloro-8-fluoropyrido[4,3-d]pyrimidine	Drug Intermediate	Others
2,4,7-Trichloro-8-fluoropyridopyrimidine is a pyridopyrimidine synthetic intermediate of MRTX1133 (HY-134813), which can be used for the synthesis of non-covalent KRAS ^G12D inhibitors .

HY-138684

MRTX9768	Histone Methyltransferase	Cancer
MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .

HY-134654

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

HY-139402

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) .

HY-139611C

Navlimetostat hydrochloride 3 Publications Verification mrtx-1719 hydrochloride; BMS-986504 hydrochloride	Histone Methyltransferase	Cancer
Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC₅₀s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .

HY-145962A

MRTX-EX185 formic	Ras	Cancer
MRTX-EX185 formic is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 formic can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 formic exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 formic also binds GDP-loaded HRAS. MRTX-EX185 formic can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-139611B

(S)-Navlimetostat (S)-mrtx-1719; (S)-BMS-986504	Histone Methyltransferase	Cancer
(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC₅₀ of 7070 nM .

HY-114436S

MRTX-1257-d6	Isotope-Labeled Compounds	Cancer
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-145962

MRTX-EX185	Ras	Cancer
MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-144323

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 .

HY-134813A

MRTX1133 formic	Ras	Cancer
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .

HY-139403

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) .

HY-137516A

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 .

HY-138684A

MRTX9768 hydrochloride	Histone Methyltransferase	Cancer
MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .

HY-160524

NOX2-IN-3	NADPH Oxidase	Cancer
NOX2-IN-3 (compound 3) is an inhibitor of NOX2 (NADPH Oxidase 2). NOX2-IN-3 sensitizes tumor cells to MRTX1133 (HY-134813) .

HY-182044

MRTX849-amide-C4-(o)-carborane	Ras Apoptosis PARP Caspase CDK	Cancer
MRTX849-amide-C4-(o)-carborane is a KRAS ^G12C inhibitor with mutation selectivity for cells expressing KRAS ^G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS ^G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS ^G12C-positive cancers .

HY-179534

G13Ci-22	Ras	Cancer
G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research .

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

Cat. No.	Product Name		Classification

HY-134813

MRTX1133 45+ Cited Publications		Alkynes
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

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 .

HY-145962A

MRTX-EX185 formic		Alkynes
MRTX-EX185 formic is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 formic can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 formic exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 formic also binds GDP-loaded HRAS. MRTX-EX185 formic can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-145962

MRTX-EX185		Alkynes
MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-179534

G13Ci-22		Alkynes
G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.