Bruton tyrosine kinase (Btk) is a member of the Tec family kinases with a well-characterized role in B-cell antigen receptor (BCR)-signaling and B-cell activation.Btk is a new target for diseases with abnormal B cell activity because it is essential for B cell development and activation through the BCR signaling pathway. The human primary immune deficiency disease X-linked agammaglobulinemia (XLA), which is caused by a mutation in the Btk gene, highlights the importance of Btk, a kinase that is only expressed in B cells and myeloid cells. The BCR signaling pathway depends on Btk in many ways.B cell receptor oligomerization, Syk and Lyn kinase activation, and Btk kinase activation are all caused by antigen binding to the BCR. When Btk is activated, it joins forces with proteins like BLNK, Lyn, and Syk to form a signaling complex that phosphorylates phospholipase C (PLC)2. This results in transcriptional changes that promote B cell survival, proliferation, and/or differentiation by releasing intracellular Ca2+ stores downstream and propagating the BCR signaling pathway through extracellular signal-regulated kinase and NF-B signaling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2494 | Pirtobrutinib | 2101700-15-4 | Pirtobrutinib (formerlyLOXO-305; LY-3527727; Jaypirca) is a novel, highly selective and non-covalent next generation BTK (Brutons tyrosine kinase) inhibitor which inhibits diverse BTK C481 substitution mutations. |
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V81226 | PROTAC BTK Degrader-5 | PROTAC BTK Degrader-5 (compound 3e) is a selective BTK degrader with DC50 of 7.0 nM in JeKo-1 cells. | |
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V39414 | QL-X-138 | 1469988-63-3 | QL-X-138 is a potent and specific BTK/MNK dual kinase inhibitor that displays covalent binding to BTK and non-covalent binding to MNK. |
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V4776 | QL47 | 1469988-75-7 | QL-47 (also known as QL-XII-47) is a novel, potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM. |
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V69498 | RSH-7 | 2764609-97-2 | RSH-7 is a potent inhibitor of BTK and FLT3 with IC50 of 47 and 12 nM respectively. |
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V4768 | Spebrutinib besylate | 1360053-81-1 | Spebrutinib (formerly known as AVL-292 and CC-292) is a novel, potent, covalent/irreversible, orally bioactive, and highly selective Btkkinase inhibitor with anIC50of 0.5 nM. |
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V69663 | TAK-020 | 1627603-21-7 | TAK-020 is a covalent/irreversible inhibitor of Btk and has become a clinical candidate active molecule. |
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V4678 | Tirabrutinib (ONO-4059) | 1351636-18-4 | Tirabrutinib (formerly ONO-4059; GS4059; ONO-WG-307; Steboronine) is a novel, potent, highly selective, covalent/irreversible and orally bioavailable BTK (Bruton agammaglobulinemia tyrosine kinase) inhibitor with anticancer activity. |
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V69662 | TL-895 | 1415823-49-2 | TL-895 is a potent, orally bioactive, ATP-competitive, selective and irreversible BTK inhibitor (antagonist) with IC50 and Kis of 1.5 nM and 11.9 nM respectively. |
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V69683 | Topoisomerase I inhibitor 11 | 2922723-28-0 | Topoisomerase I inhibitor 11 is a potent inhibitor of topoisomerase I. |
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V3979 | ZANUBRUTINIB | 1691249-45-2 | Zanubrutinib (formerly known as BGB-3111), an S-enantiomer, is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers. |
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V78693 | Zanubrutinib-d5 (BGB-3111 d5) | Zanubrutinib-d5 is the deuterated form of Zanubrutinib. |
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