2. Signaling Pathways
  3. GPCR/G Protein
    MAPK/ERK Pathway
  4. Ras
  5. K-Ras Isoform

K-Ras

 

K-Ras Related Products (140):

Cat. No. Product Name Effect Purity
  • HY-114277
    Sotorasib
    		Inhibitor 99.94%
    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-134813
    MRTX1133
    		Inhibitor 99.42%
    MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD 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
    		Inhibitor 99.93%
    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-148439
    RMC-6236
    		Inhibitor 99.88%
    RMC-6236 (Compound A122) is a potent RAS(ON)MULTI inhibitor and can be used for the research of cancer.
  • HY-156498
    RMC-7977
    		Inhibitor 99.48%
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRASG12C cancer models, and demonstrates good tolerability across various RAS cancer models.
  • HY-159127
    HRS-4642
    		Inhibitor
    HRS-4642 is a selective KRAS(G12D) inhibitor (Kd=0.083 nM) with anti-cancer activity. HRS-4642 synergizes with Carfilzomib (HY-10455) and exhibits significant in vivo potency to reshape the tumor microenvironment into an immune-activating microenvironment.
  • HY-163595
    Pan-RAS-IN-4
    		Inhibitor
    Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC50 of ＜ 100 nM for KRAS G12D. Pan-RAS-IN-4 plays an important rile in cancer research.
  • HY-159163
    KRASG12C IN-12
    		Inhibitor
    KRASG12C IN-12 (compound-1) is a KRASG12C inhibitor. KRASG12C IN-12 (compound-1) can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant.
  • HY-125817
    BI-3406
    		Inhibitor 99.95%
    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
  • HY-126247
    BI-2852
    		Inhibitor 99.57%
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-145928
    Divarasib
    		Inhibitor 99.46%
    Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
  • HY-156819
    RMC-9805
    		Inhibitor 99.73%
    RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRAS G12D mutant cancer cells.
  • HY-153346
    RMC-6291
    		Inhibitor 99.65%
    RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM.
  • HY-145926
    MRTX0902
    		Inhibitor 99.75%
    MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
  • HY-137516
    LC-2
    		Inhibitor 98.04%
    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-114398
    BAY-293
    		Inhibitor 98.91%
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-139612
    Opnurasib
    		Inhibitor 98.94%
    Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.
  • HY-U00418
    ARS-1620
    		Inhibitor 99.62%
    ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.
  • HY-114277A
    Sotorasib racemate
    		Inhibitor 98.99%
    Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research.
  • HY-148098
    Pan KRas-IN-1
    		Inhibitor 98.47%
    Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors.