BTK
BTK (Bruton's tyrosine kinase) binds PIP3 and phosphorylates phospholipase C, plays a crucial role in B cell maturation as well as mast cell activation.
Products for BTK
- Cat.No. Product Name Information
- GC34069 (±)-Zanubrutinib ((±)-BGB-3111) (±)-Zanubrutinib ((±)-BGB-3111) ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
- GC67857 (R)-Elsubrutinib
- GC63797 (S)-Sunvozertinib (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
- GC60551 Acalabrutinib D4
- GC15453 ACP-196 ACP-196 (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. ACP-196 binds covalently to Cys481 in the ATP-binding pocket of BTK. ACP-196 demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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GC31679
ARQ 531
ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
- GC13562 AVL-292 A covalent BTK inhibitor
- GC63846 BIIB091 BIIB091 is a highly selective, reversible and orally active BTK inhibitor for treating autoimmune diseases.
- GC68373 BLK-IN-2
- GC31760 BMS-935177 BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
- GC31713 BMS-986142 A BTK inhibitor
- GC32844 BMS-986195 BMS-986195 (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 of 0.1 nM.
- GC11063 BMX-IN-1 A selective BMX and BTK inhibitor
- GC19333 BTK IN-1 BTK IN-1 is a potent BTK inhibitor, with an IC50 of <100 nM.
- GC35561 Btk inhibitor 1 Btk inhibitor 1 is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
- GC35562 Btk inhibitor 1 hydrochloride
- GC10924 Btk inhibitor 1 R enantiomer Btk inhibitor 1 R enantiomer is an impurity of Ibrutinib. Btk inhibitor 1 R enantiomer can be used in synthesis of Btk inhibitor 1 R enantiomer Ibrutinib dimer and Btk inhibitor 1 R enantiomer adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
- GC35563 Btk inhibitor 1 R enantiomer hydrochloride Btk inhibitor 1 R enantiomer hydrochloride is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
- GC67940 BTK inhibitor 10
- GC62498 BTK inhibitor 17 BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM.
- GC64360 BTK inhibitor 18 BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM.
- GC32007 Btk inhibitor 2 Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
- GC33064 CG-806 (Luxeptinib) CG-806 (Luxeptinib) (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. CG-806 (Luxeptinib) induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
- GC13365 CGI-1746 A potent, selective BTK inhibitor
- GC35683 CHMFL-BTK-01 CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC50 of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation.
- GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
- GC13439 CNX-774 BTK inhibitor, orally active, irreversible and selective
- GC64819 Elsubrutinib Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM.
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GC34062
Evobrutinib (M2951)
Evobrutinib, as an orally, highly selective, covalent Bruton's tyrosine kinase inhibitor, was well‐tolerated and effective.
- GC11995 GDC-0834 GDC-0834 is the S-enantiomer of GDC-0834.
- GC36127 GDC-0834 Racemate Racemic form of GDC-0834
- GC19162 GDC-0853 GDC-0853 (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. GDC-0853 has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
- GC39194 Ibrutinib D5 Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
- GC60197 Ibrutinib deacryloylpiperidine Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
- GC36289 Ibrutinib-biotin Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
- GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor
- GC36661 MT-802 MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM.
- GC62255 N-piperidine Ibrutinib hydrochloride N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
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GC69600
NX-2127
NX-2127 is an orally effective BTK inhibitor that can induce the degradation of mutated BTKC481S in cells. NX-2127 inhibits the proliferation of TMD8 cells with the BTKC481S mutation more effectively than Ibrutinib. NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3), corresponding to concentrations of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells.
- GC13219 ONO-4059 ONO-4059 is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor.
- GC36861 PCI 29732 A multi-kinase inhibitor
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GC13812
PCI-32765 (Ibrutinib)
PCI-32765 (Ibrutinib) is an irreversible selective inhibitor of Bruton s tyrosine kinase (BTK) that selectively targets its kinase domain.
- GC12921 PCI-32765 Racemate PCI-32765 Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
- GC30155 PCI-33380 PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
- GC34709 PF-06250112 PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively.
- GC62515 Pirtobrutinib Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.
- GC31339 PRN1008 PRN1008 (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton's Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
- GC37048 QL47 QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses.
- GC38375 Remibrutinib Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM.
- GC11230 RN486 Btk inhibitor,potent and selective
- GC62614 SJF620 hydrochloride SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
- GC37672 Spebrutinib besylate Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.
- GC64120 TAK-020 TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
- GC33821 Tirabrutinib (ONO-4059) Tirabrutinib (ONO-4059) (ONO-4059) is an orally active Bruton's Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM.
- GC34097 Tirabrutinib hydrochloride (ONO-4059 (hydrochloride)) Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton's Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM.
- GC63229 TL-895 TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively.
- GC63232 Tolebrutinib Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.
- GC34077 Vecabrutinib (SNS-062) Vecabrutinib (SNS-062) (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib (SNS-062) shows an IC50 of 24 nM for ITK.
- GC34075 Zanubrutinib (BGB-3111) Zanubrutinib (BGB-3111) (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.