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RET+inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112301
    Pralsetinib
    15+ Cited Publications

    BLU-667

    		 RET Cancer
    Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
    Pralsetinib
  • HY-18840
    BBT594
    2 Publications Verification

    NVP-BBT594

    		 RET Cancer
    BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
    BBT594
  • HY-132846
    Vepafestinib

    TAS0953/HM06

    		 RET Apoptosis Cancer
    Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas .
    Vepafestinib
  • HY-112301A
    trans-Pralsetinib

    trans-BLU-667

    		 RET Cancer
    trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129 .
    trans-Pralsetinib
  • HY-151377
    RET-IN-19

    		RET EGFR Aurora Kinase c-Fms MAP4K Cancer
    RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research .
    RET-IN-19
  • HY-146710
    RET-IN-16

    		RET Cancer
    RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects .
    RET-IN-16
  • HY-178061
    APS03118

    		ERK RET Cancer
    APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
    APS03118
  • HY-174245
    RET-IN-30

    		RET Cancer
    RET-IN-30 (Compound 28) is a RET inhibitor that exhibits inhibitory activity against both wild-type RET and some of its mutants. RET-IN-30 can inhibit the proliferation of A549 cells and has anti-tumor activity .
    RET-IN-30
  • HY-153676
    RET-IN-23

    		RET Cancer
    RET-IN-23 (compound 17) is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. RET-IN-23 shows anti-tumor activity .
    RET-IN-23
  • HY-112301R
    Pralsetinib (Standard)

    BLU-667 (Standard)

    		 Reference Standards RET Cancer
    Pralsetinib (Standard) is the analytical standard of Pralsetinib. This product is intended for research and analytical applications. Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
    Pralsetinib (Standard)
  • HY-144030
    RET-IN-12

    		RET Others
    RET-IN-12 (compound 2) is a RET inhibitor, with IC50 values of 0.3 nM and 1 nM for RET(WT) and RET(V804M), respectively .
    RET-IN-12
  • HY-112301AR
    trans-Pralsetinib (Standard)

    trans-BLU-667 (Standard)

    		 RET Reference Standards Cancer
    trans-Pralsetinib (Standard) is the analytical standard of trans-Pralsetinib. This product is intended for research and analytical applications. trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129 .
    trans-Pralsetinib (Standard)
  • HY-151987
    RET-IN-20

    		RET Apoptosis Cancer
    RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity .
    RET-IN-20
  • HY-144029
    RET-IN-13

    		RET Cancer
    RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research .
    RET-IN-13
  • HY-168868
    RET ligand-2

    		RET Ligands for Target Protein for PROTAC Cancer
    RET ligand-2 is a selective RET inhibitor. RET ligand-2 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC RET degraders with antitumor activity. RET ligand-2 can be used for the synthesis of RD-23 (HY-168867) .
    RET ligand-2
  • HY-149451
    SYHA1815

    		RET VEGFR c-Myc Cancer
    SYHA1815 is an orally active RET inhibitor (IC50=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC50=15.9 nmol/L). SYHA1815 arrests the G1 cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc .
    SYHA1815
  • HY-144170
    RET-IN-14

    		RET Btk Cancer
    RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
    RET-IN-14
  • HY-144131
    RET-IN-11

    		Apoptosis RET Cancer
    RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RET V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis .
    RET-IN-11
  • HY-149099
    RET-IN-22

    		RET Cancer
    RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
    RET-IN-22
  • HY-132193
    RET-IN-4

    		RET Cancer
    RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects .
    RET-IN-4
  • HY-178786
    RET-IN-31

    		RET Potassium Channel Cytochrome P450 Cancer
    RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RET WT, RET V804L, RET V804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers .
    RET-IN-31
  • HY-170926
    CQ1373

    		RET Apoptosis Cancer
    CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
    CQ1373
  • HY-183729
    RET-IN-34

    		Ligands for Target Protein for PROTAC RET Endocrinology Cancer
    RET-IN-34 (Compound EV1) is a RET inhibitor with an IC50 of 0.89 nM. RET-IN-34 serves as a target protein ligand for PROTAC synthesis (Ligand for Target Protein for PROTAC). RET-IN-34 is applicable for the synthesis of PROTAC RET Degrader 2 (HY-183783). RET-IN-34 exhibits anticancer activity against medullary thyroid carcinoma. RET-IN-34 can be used in studies related to medullary thyroid carcinoma .
    RET-IN-34
  • HY-182741
    RET-IN-32

    		RET Endocrinology Cancer
    RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer .
    RET-IN-32

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