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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V69682 | (R)-Elsubrutinib ((R)-ABBV-105) | 1643570-23-3 | (R)-Elsubrutinib ((R)-ABBV-105) is a Btk inhibitor. |
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V69668 | (R)-Pirtobrutinib ((R)-LOXO-305) | 2101700-14-3 | (R)-Pirtobrutinib is the less active isomer of Pirtobrutinib. |
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V3391 | (R)-Zanubrutinib | 1691249-44-1 | R)-Zanubrutinib is the R-enantiomer of Zanubrutinib (formerly known as BGB-3111) which is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers. |
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V69702 | (Rac)-IBT6A hydrochloride ((Rac)-ibrutinib) | 1807619-60-8 | (Rac)-IBT6A HCl is the racemate of IBT6A HCl. |
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V69691 | (Rac)-PF-06250112 | 1609465-88-4 | (Rac)-PF-0625011 is the racemate of PF-06250112. |
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V3392 | (±)-Zanubrutinib | 1633350-06-7 | Zanubrutinib is a racemic mixture of Zanubrutinib (formerly known as BGB-3111) which is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers. |
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V2980 | Acalabrutinib (ACP-196) | 1420477-60-6 | Acalabrutinib (formerly known as ACP196; ACP-196; trade name:Calquence)is a selective second-generation Brutons tyrosine kinase (BTK) inhibitor with anticancer activity. |
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V69669 | Acalabrutinib-d4 (ACP-196-d4) | 2699608-18-7 | Acalabrutinib-d4 is a deuterated form of Acalabrutinib. |
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V69667 | Atuzabrutinib (SAR 444727; PRN473) | 1581714-49-9 | Atuzabrutinib (SAR 444727) is a potent, selective and reversible Btk inhibitor. |
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V69689 | BCPyr | 2669844-82-8 | BCPyr is a new candidate BTK degrader (DC50 = 800 nM). |
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V69672 | BGB-8035 | 2283349-24-4 | BGB-8035 is an orally bioactive and selective BTK inhibitor (antagonist) with IC50s of 1.1 nM, 99 nM and 621 nM for BTK, TEC and EGFR respectively. |
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V69660 | BLK-IN-2 | 2694871-86-6 | BLK-IN-2 (compound 25) is a specific and irreversible inhibitor of B-lymphoid tyrosine kinase (BLK) with IC50 of 5.9 nM. |
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V3184 | BMS-935177 | 1231889-53-4 | BMS-935177 is a potent, selective, reversible, and 2nd generation inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 3 nM. |
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V4066 | BMS-986142 | 1643368-58-4 | BMS-986142, a carbazole and tetrahydrocarbazole based compound, is a novel, potent and highly selective reversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 0.5 nM. |
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V69679 | BMS-986143 | 1643372-83-1 | BMS-986143 is an orally bioactive, reversible BTK inhibitor (antagonist) with IC50 of 0.26 nM. |
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V3807 | BMS-986195 | 1912445-55-6 | Branebrutinib (formerly BMS-986195) is a highly selective and rapidly acting covalent/irreversible inhibitor of Bruton’s Tyrosine Kinase (BTK) with IC50 of<1 nM and robust efficacy at low doses in preclinical models of RA (Rheumatoid Arthritis) and Lupus Nephritishighly. |
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V4782 | BMX-IN-1 | 1431525-23-3 | BMX-IN-1 is a novel, potent, selective and covalent / irreversible BMX (bone marrow tyrosine kinase on chromosome X) inhibitor with the potential for treating prostate cancer. |
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V4766 | BTK IN-1 | 1270014-40-8 | BTK IN-1 (SNS-062 analog or Vecabrutinib analog) is a novel and potent BTK (Bruton's tyrosine kinase) inhibitor with an IC50 of<100 nM. |
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V32618 | Btk inhibitor 1 R enantiomer hydrochloride | 1553977-42-6 | Btk inhibitor 1 R-enantiomer hydrochloride (IBT6A hydrochloride), the R-isomer and hydrochloride salt form of Btk inhibitor 1, is a novel and potent Bruton's tyrosine kinase (BTK) inhibitor with potential antitumor activity. |
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V69673 | BTK inhibitor 13 | 2376726-26-8 | BTK inhibitor 13 (compound 8) is a potent and specific (BTK) inhibitor (antagonist) with IC50 of 1.2 nM. |
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