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wild-type BTK

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153321
    Bexobrutideg
    1 Publications Verification

    NX-5948; BTK-IN-24

    		 PROTACs Btk Inflammation/Immunology Cancer
    Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    Bexobrutideg
  • HY-19816
    Avitinib
    3 Publications Verification

    Abivertinib; AC0010

    		 EGFR Btk Apoptosis Cancer
    Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .
    Avitinib
  • HY-19816A
    Avitinib maleate
    3 Publications Verification

    Abivertinib maleate; AC0010 maleate

    		 EGFR Btk Apoptosis Cancer
    Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .
    Avitinib maleate
  • HY-122562
    MT-802
    4 Publications Verification

    		 PROTACs Btk Cancer
    MT-802 is a BTK PROTAC degrader. MT-802 degrades wild-type BTK (DC50 = 14.6 nM) and BTK mutants including E41K, C481S (DC50 = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997)-resistant chronic lymphocytic leukemia (CLL). (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340)) .
    MT-802
  • HY-156640
    Rocbrutinib

    LP-168

    		 EGFR Cancer
    Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma .
    Rocbrutinib
  • HY-160142
    UBX-382

    		PROTACs Btk Syk MEK ERK Cancer
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
    UBX-382
  • HY-153803
    GBD-9

    		PROTACs Molecular Glues Btk Cancer
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
    GBD-9
  • HY-174850
    CFON-026

    		Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-175541
    TQ-3959

    		PROTACs Btk Cancer
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
    TQ-3959
  • HY-147580
    BTK-IN-10

    		Btk Cancer
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
    BTK-IN-10
  • HY-153321A
    (R,R)-Bexobrutideg

    (R,R)-NX-5948; (R,R)-BTK-IN-24

    		 Drug Isomer PROTACs Btk Inflammation/Immunology Cancer
    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    (R,R)-Bexobrutideg
  • HY-169228
    WS-11

    		Btk Cancer
    WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
    WS-11
  • HY-147582
    BTK-IN-12

    		Btk Cancer
    BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
    BTK-IN-12
  • HY-W591307
    P131

    		PROTAC Linkers Cancer
    P131 is a PROTAC molecule comprised of Pomalidomide-based cereblon ligand and IBT6A, linked by a PEG 3 chain. P131 can degrade both wild-type and C481S mutant BTK with nanomolar potencies.
    P131
  • HY-168427
    Avitinib maleate dihydrate

    Abivertinib maleate dihydrate; AC0010 maleate dihydrate

    		 EGFR Btk Apoptosis Cancer
    Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects .
    Avitinib maleate dihydrate
  • HY-124153
    GNE-431

    		Btk Cardiovascular Disease Inflammation/Immunology
    GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
    GNE-431
  • HY-151211
    BTK-IN-16

    		Btk Inflammation/Immunology Cancer
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
    BTK-IN-16
  • HY-160167A
    (R,R)-Birelentinib

    (R,R)-DZD8586

    		 Btk Cancer
    (R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies .
    (R,R)-Birelentinib
  • HY-181547
    HBC-12551

    		Btk Cancer
    HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTK C481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma .
    HBC-12551

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