BTK

<p>GDC-0834, the S-enantiomer, is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK).</p>

<p>CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases).</p>

<p>Tilfrinib is an effective and selective inhibitor of breast tumor kinase(Brk, IC50 = 3.15 nM) which displays anti-proliferative and anti-tumor activities.</p>

<p>NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative</p>

<p>(±)-Zanubrutinib ((±)-BGB-3111) is a potent and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability,</p>

<p>(R)-Zanubrutinib ((R)-BGB-3111) is a selective inhibitor of Bruton tyrosine kinase (BTK).</p>

<p>(Rac)-PF-0625011 is a racemic mix, orally active, selective BTK inhibitor, also targeting BMX and TEC kinases.</p>

<p>BTK-IN-19 is a reversible BTK inhibitor with an IC 50 of &lt;0.001 μM .</p>

<p>BTK inhibitor 20 is a potent BTK inhibitor with an IC 50 of 8 nM .</p>

<p>BTK-IN-18 is a potent, reversible inhibitor of Bruton's tyrosine kinase (BTK) with an inhibitory concentration (IC50) of 0.002 µM.</p>

<p>BTK-IN-17: selective, oral BTK inhibitor, IC50=13.7 nM, reduces p-BTK Y223/p-PLCγ2 Y1217, anti-inflammatory.</p>

<p>BTK-IN-11: potent BTK inhibitor; may research autoimmune, inflammatory diseases, cancer. (Patent WO2022063101A1, Z2)</p>

<p>PF-303, a reversible covalent BTK inhibitor, shows potential for cancer and autoimmune therapy.</p>

<p>BTK inhibitor 13 (compound 8) is an effective and selective BTK inhibitor(IC50: 1.2 nM).</p>

<p>Pirtobrutinib: a selective, non-covalent BTK inhibitor effective against BTK C481 mutations, causing tumor regression in lymphoma models.</p>

<p>Cinsebrutinib, a Bruton's tyrosine kinase inhibitor, holds potential for research in cancer treatment.</p>

<p>Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity and is used in the treatment of tumors, immune system disorders, and blood and</p>

<p>BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton’s tyrosine</p>

<p>PF-06250112 is an effective and highly selective BTK inhibitor (IC50: 0.5 nM.</p>

<p>TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases.</p>

<p>BTK inhibitor 1 (Compound 27) is a BTK inhibitor (IC50: 0.11 nM) with an inhibitory effect on B-cell activation in hWB with an IC50 of 2 nM.</p>

<p>BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.</p>

<p>WS-11 is a non-covalent reversible inhibitor of BTK, with IC50 values of 3.9 nM for the wild-type and 2.2 nM for the C481S mutant BTK. In addition to strong hydrogen bonding, WS-11 also forms robust π-π interactions with PHE540, and p-π interactions with LYS430 within the active pocket.</p>

<p>BTK-IN-38 (Example 125) is an efficacious inhibitor of BTK. It effectively suppresses the proliferation of DOHH2 and BT474 cells, with IC50 values of 114 nM and 340 nM, respectively.</p>

<p>JAK3/BTK-IN-4, a dual inhibitor for JAK3/BTK, shows synergy in autoimmune disease treatment. (Patent WO2021147953A1, compound 003)</p>

<p>GNE-431: potent, selective noncovalent Btk inhibitor, IC50=3.2 nM; effective against C481R, T474I, T474M mutants, may counter ibrutinib resistance.</p>

<p>BIIB129 is a selective and brain-penetrant BTK covalent inhibitor used to study B-cell proliferation-related diseases.</p>

<p>BTK-IN-15: Oral BTK inhibitor, IC50 0.7 nM, induces cancer cell apoptosis, selective with anti-tumor effects.</p>

<p>RET-IN-14 inhibits RET (IC50: &lt;0.51-9.3 nM) &amp; BTK (C481S) (IC50: 9.2-15 nM), promising for tumor research.</p>

<p>BMS-986143: oral BTK inhibitor, IC50=0.26 nM, potential for autoimmune research, also targets TEC, BLK, BMX, TXK, YES1, ITK.</p>

<p>BTK-IN-16 is a potential inhibitor of wild-type BTK and C481S mutants.BTK-IN-16 can be used to study various autoimmune diseases and cancers caused by BTK.</p>

<p>BTK inhibitor 18 is a selective, potent, covalent, orally active Btk inhibitor (IC50: 142 nM) that exhibits anti-inflammatory effects.</p>

<p>G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM).</p>

<p>JAK3/BTK-IN-3: strong dual JAK3/BTK suppressor, promising for autoimmune disease research.</p>

<p>BTK-IN-10 is a potent inhibitor of BTK, acting on wild-type BTK (IC50&lt;5 nM) or mutant BTK (C481S) (IC50&lt;5 nM).</p>

<p>HDHD4-IN-1 (compound 3) is an inhibitor of N-acetylneuraminate-9-phosphate phosphatase (HDHD4) with an IC50 value of 11 μM. It is utilized in the research of neurological disorders.</p>

<p>JAK3/BTK-IN-7 (XL-12), characterized as a JAK3/BTK inhibitor, exhibits IC 50 values of 2 nM and 14 nM for JAK3 and BTK respectively. This compound demonstrates anti-inflammatory properties and is applicable in research related to rheumatoid arthritis [1].</p>

<p>Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins with an IC50 value of 0.22 μM for T24 cell proliferation. It also suppresses T24 cell migration and colony formation in a dose-dependent manner, induces G1 phase arrest, and triggers apoptosis. By targeting BMX proteins, it inhibits the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, while also inhibiting Arf1 proteins to eliminate bladder cancer stem cells and activate antitumor immunity, thus exhibiting anticancer activity. Brefeldin A 4-O-nicotinate is applicable in research related to bladder cancer.</p>

<p>BTK-IN-8: potent, selective covalent BTK inhibitor; IC50=0.22 nM, Kd=0.91 nM; effective in blood CD69 cells (IC50=0.029 μM).</p>

<p>BTK-IN-6, a potent BTK inhibitor, may treat immune, cardiac, cancer, viral, inflammatory, metabolic, and neurological disorders.</p>

<p>Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.</p>

<p>PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A.<br>1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)</p>

<p>BTK-IN-25 (compound 71) is a potent BTK inhibitor, demonstrating an IC50 of 0.77 nM against BTK(C481S) and achieving an IC50 of 1 nM in DOHH2 cells [1].</p>

<p>JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier.</p>

<p>BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM.</p>