Kras

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.BI-2493 exhibits antitumor activity and inhibits tumor cell growth and can be used in the study of cancerous diseases.BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.

Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.

RMC-9805 is a potent KRAS G12D inhibitor with potential anti-tumor and inhibitory activity against tumor cell proliferation for the study of pancreatic cancer.

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

BI-2852 is a KRAS inhibitor targeting the switch I II pocket (SI II-pocket) with nanomolar affinity, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.

ARS-1620 is a covalent inhibitor of K-RASG12C.

Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.

(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors.

AZD4747 is a selective and potent inhibitor of the mutant GTPase KRASG12C that crosses the blood-brain barrier and has potential antitumor activity for the study of pancreatic and colorectal adenocarcinoma.

Garsorasib is an effective KRAS G12C inhibitor (IC50 = 10 nM) and can be used in studies about cancer treatment.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

3344 is an inhibitor of KRAS-effector interactions，with an affnity of 126nm.

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.

Kras4B G12D-IN-1 is an anticancer agent that functions as an inhibitor of the Kras4B G12D protein. It effectively reduces the expression of Kras protein in mouse embryonic fibroblasts (MEFs) harboring the Kras4B G12D mutation[1].

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK PD experiment.

GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) is a high kinase-selective inhibitor of RAF and targets KRAS-mutant cancers through combination therapy.

ASP2453 is a potent, selective, and covalent inhibitor of KRAS G12C that inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.

6H05 TFA (6H05 trifluoroacetate) is a selective, and allosteric oncogenic mutant K-Ras(G12C) inhibitor.

Compound 3344 hydrochloride is an inhibitor of KRAS-effector interactions，with an affnity of 126nM.

KRAS G12C inhibitor 16 is a potent inhibitor of KRAS G12C.

1588-A4 (ARS-1620 Intermediate) is an intermediate of ARS-1620 which is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.

ARS-1630 is a mutant K-ras G12C inhibitor. It is a less active enantiomer of ARS-1620.

ARS-1323 is the racemate of ARS-1620 and a mutant K-ras G12C inhibitor.

K-Ras G12C-IN-4, is a potent Covalent Inhibitor of KRASG12C..

BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model. activity.BI-0474 can be used for cancer research.

ARS-1323-alkyne is a switch-II pocket (S-IIP) inhibitor and a conformational specific chemical reporter of KRASG12C nucleotide state in living cells.

(S)-BAY-293 is a potent pan-KRAS inhibitor used in the study of primary non-small cell lung and pancreatic cancers.

KRAS G12C inhibitor 19 is a potent KRAS G12C inhibitor that demonstrates anti-tumor activity in cellular assays and inhibits tumor growth [1].