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Results for "

KRASG12D inhibitor

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

2

Isotope-Labeled Compounds

8

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-173637
    AZD0022

    		Ras Cancer
    AZD0022 is a selective and orally active KRAS G12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model .
    AZD0022
  • HY-126247
    BI-2852

    		Ras Cancer
    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.
    BI-2852
  • HY-153663
    TH-Z827

    		Ras Cancer
    TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
    TH-Z827
  • HY-171255
    KRAS G12D inhibitor 26

    		Ras Cancer
    KRAS G12D inhibitor 26 is a modulator of Kras, targeting Kras(G12D) with an IC50 ≤ 100 nM .
    KRAS G12D inhibitor 26
  • HY-157029S
    KRASG12D-IN-1

    		Ras Cancer
    KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-1
  • HY-162445
    KRASG12D-IN-3

    		Ras PERK Cancer
    KRASG12D-IN-3 is an orally active KRAS G12D inhibitor. KRASG12D-IN-3 inhibits the growth of gastric cancer and pancreatic cancer cells. KRASG12D-IN-3 inhibits the activity of p-ERK in gastric cancer cells. KRASG12D-IN-3 can be used for the research of gastric cancer and pancreatic cancer .
    KRASG12D-IN-3
  • HY-157031S
    KRASG12D-IN-2

    		Ras Cancer
    KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-2
  • HY-126247B
    (R)-BI-2852

    		Drug Derivative Ras Cancer
    (R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. 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.
    (R)-BI-2852
  • HY-179300A
    KRAS-IN-48

    		Ras Cancer
    KRAS-IN-48 (Compound 1-01) is a KRAS mutant inhibitor, with Kd values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer .
    KRAS-IN-48
  • HY-163488
    KRASG12D-IN-4

    		Ras Cancer
    KRASG12D-IN-4 (example 38) is a KRas G12D inhibitor with an IC50 of 3.3 nM. KRASG12D-IN-4 inhibits proliferation of pancreatic cancer ASPC-1 cells with an IC50 of 12 nM .
    KRASG12D-IN-4
  • HY-174243
    KRASG12D-IN-5

    		Ras Cancer
    KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. KRASG12D-IN-5 has potent anticancer activity with no significant cytotoxicity against BxPC-3 (WT), KRAS mutation AsPC-1 (G12D) and MIAPaCa-2 cells (G12C) with CC50s of 10.37, 0.76 and 0.3 μM, respectively. KRASG12D-IN-5 can be used for cancer research, such as lung, pancreatic and colorectal cancer .
    KRASG12D-IN-5
  • HY-175529
    KRASG12D-IN-7

    		Ras ERK Apoptosis Cancer
    KRASG12D-IN-7 is a selective KRAS G12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRAS G12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRAS G12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRAS G12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC) .
    KRASG12D-IN-7
  • HY-158007
    (RS)-G12Di-1

    		Ras Cancer
    (RS)-G12Di-1 is a selective, covalent inhibitor of K-Ras-G12D .
    (RS)-G12Di-1
  • HY-163594
    KRAS-IN-59

    		Ras Cancer
    K-Ras-IN-58 is a K-RAS inhibitor and shows inhibitory activity against KRASG12D, KRASG12C and KRAS WT. K-Ras-IN-58 inhibits proliferation of cancer cells .
    KRAS-IN-59
  • HY-173329
    KRAS-IN-41

    		Ras Cancer
    KRAS-IN-41 is an inhibitor of KRAS with IC50 values of <0.01 μM for KRAS G12D and KRAS G12V. KRAS-IN-41 inhibits RAS mutant cell lines, GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS-IN-41 can be used in cancer research .
    KRAS-IN-41
  • 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 KD 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 .
    MRTX1133 formic
  • HY-176419
    KRAS inhibitor-42

    		Ras Cancer
    KRAS inhibitor-42 (compound 8) is a potent USP7 inhibitor. KRAS inhibitor-42 has high affinity against GDP-bound KRASG12D with a Ki of 2.7 μM .
    KRAS inhibitor-42
  • HY-184010
    KRASG12D-IN-8

    		Ras ERK Cancer
    KRASG12D-IN-8 is an orally active KRAS G12D inhibitor, with a Kd value of 0.003 nM for KRAS G12D and 0.024 nM for KRAS G12V. KRASG12D-IN-8 inhibits the activity of phosphorylated ERK in KRAS-mutated cells. KRASG12D-IN-8 induces tumor regression in ovarian cancer xenograft mouse models. KRASG12D-IN-8 can be used for the research of KRAS-mutated cancers .
    KRASG12D-IN-8
  • HY-180200
    RNK08954

    		Ras ERK Cancer
    RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
    RNK08954
  • HY-180920
    KRAS G12D-IN-36

    		Ras ERK Cancer
    KRAS G12D-IN-36 (Compound 53a) is a highly selective and orally active KRAS-G12D inhibitor with an IC50 of 1.63 nM. KRAS G12D-IN-36 effectively inhibits p-ERK with an IC50 of 8.4 nM. KRAS G12D-IN-36 shows potent anti-proliferative activity against AsPC-1 cells. KRAS G12D-IN-36 can be used for research on pancreatic cancer .
    KRAS G12D-IN-36

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