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Results for "

KM12

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-164514
    NMS-P626

    		Trk Receptor Cancer
    NMS-P626 is an inhibitor of TRKA, TRKB, and TRKC, with IC50 values of 8 nM, 7 nM, and 3 nM, respectively. NMS-P626 inhibits the growth of KM12 cells by suppressing the phosphorylation of TPM3-TRKA and downstream signaling in KM12 cells, with an IC50 of 19 nM for KM12 cells. NMS-P626 can be used in colorectal cancer research .
    NMS-P626
  • HY-144321
    Trk-IN-9

    		Trk Receptor Cancer
    Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
    Trk-IN-9
  • HY-137465
    CG428

    		Trk Receptor Cancer
    CG428 is a potent and selective tropomyosin receptor kinase (TRK) degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM) .
    CG428
  • HY-161775
    RET/TRKA-IN-1

    		RET Trk Receptor Cancer
    RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase .
    RET/TRKA-IN-1
  • HY-163004
    Type II TRK inhibitor 2

    		Trk Receptor Cancer
    Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
    Type II TRK inhibitor 2
  • HY-164517
    ONO-7579

    		Trk Receptor Cancer
    ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research .
    ONO-7579
  • HY-131244
    ALK-IN-9

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .
    ALK-IN-9
  • HY-133739
    NBD-125

    		RAR/RXR Cancer
    NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell .
    NBD-125
  • HY-157542
    CG428-NEG

    		Others Others
    CG428-NEG is a TRK degrader negative control. CG428-NEG inhibits cell growth and reduce TPM3-TRKA levels .
    CG428-NEG
  • HY-12678R
    Entrectinib (Standard)

    		ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib (Standard)
  • HY-12678
    Entrectinib
    20+ Cited Publications

    NMS-E628; RXDX-101

    		 ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib
  • HY-12678S1
    Entrectinib-d8

    NMS-E628-d8; RXDX-101-d8

    		 Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase Cancer
    Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
    Entrectinib-d8
  • HY-102066
    Utatrectinib

    AZD-7451

    		 Trk Receptor Cancer
    Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
    Utatrectinib

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