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BTK
BTK製品
- All (40)
- BTK阻害剤 (39)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| S2680 | Ibrutinib | イブルチニブ (Ibrutinib (PCI-32765)) は、無細胞アッセイで IC50 が 0.5 nM の強力で選択性の高い Brutons チロシンキナーゼ (Brutons tyrosine kinase, Btk) 阻害剤であり、Bmx, CSK, FGR, BRK, HCKに対しても阻害活性を持ちます。 EGFR, Yes, ErbB2, JAK3 に対しては前者より比較的弱い活性を持ちます。イブルチニブは、P13I を含む一連の PROTAC の合成における Btk リガンドとして適用できます。 |
|
|
| S8116 | Acalabrutinib (ACP-196) | Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR. |
|
|
| S7173 | Spebrutinib (AVL-292) | Spebrutinib (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1. |
|
|
| S8166 | tirabrutinib(ONO-4059) hydrochloride | Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. | ||
| S7051 | CGI1746 | CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
|
|
| S7734 | LFM-A13 | LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK. |
|
|
| S7257 | CNX-774 | CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
|
|
| S8294 | Olmutinib (BI 1482694) | Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase. | ||
| S8348 | BMS-935177 | BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. | ||
| S8421 | Fenebrutinib (GDC-0853) | Fenebrutinib (GDC-0853) is a potent, selective, and non-covalent bruton's tyrosine kinase (BTK) inhibitor with an Ki value of 0.91 nM for Btk with >100-fold selectivity over 3 off-targets (Bmx :153-fold, Fgr: 168-fold, Src:131-fold). | ||
| S8832 | Branebrutinib (BMS-986195) | Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. | ||
| S8741 | Avitinib (Abivertinib) | Avitinib (Abivertinib) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. | ||
| S8381 | BMS-986142 | BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX). | ||
| S8791 | Zanubrutinib | Zanubrutinib is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR. | ||
| S8711 | Nemtabrutinib (ARQ 531) | Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. | ||
| S9825 | Pirtobrutinib (LOXO-305) | Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases. | ||
| S7080 | RN486 | RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM. | ||
| S8679 | BTK inhibitor 1 (Compound 27) | BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. | ||
| E1381 | NX-2127 | NX-2127 is a unique, potent inhibitor of BTK that prevents its functions by catalyzing the ubiquitylation and proteasomal degradation of BTK rather than via direct binding. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells. | ||
| S7877 | ONO-4059 analogue | ONO-4059 analogue (ONO-WG-307) is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1. | ||
| E2838 | M7583 | M7583 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with IC50 and Ki of 1.5 nM and 11.9 nM, respectively. | ||
| E1660New | NX-5948 | NX-5948(BTK-IN-24) is a novel oral small molecule that induces BTK degradation via cereblon E3 ubiquitin ligase recruitment. It mediates potent anti-inflammatory activity and can cross the blood-brain barrier in animal models. | ||
| E2843 | Poseltinib | Poseltinib (HM71224, LY3337641) shows a highly selective inhibition for Bruton’s tyrosine kinase (BTK) with IC50 of 1.95 nM, in which the selectivity toward other BMX, TEC and TXK are 0.3, 2.3 and 2.4 fold, respectively. | ||
| E1848New | BGB-8035 | BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. BGB-8035 exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases. | ||
| E1582New | Edralbrutinib | Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL). | ||
| E1611New | Atuzabrutinib | Atuzabrutinib (SAR 444727, PRN473) is a reversible, selective inhibitor of Bruton's tyrosine kinase (Btk). It can effectively prevent neutrophil recruitment via inhibition of macrophage antigen‐1 signalling. | ||
| S6966 | MT-802 | MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL). | ||
| E1355New | JNJ-64264681 | JNJ-64264681 is an orally active, irreversible covalent inhibitor of Bruton's tyrosine kinase (BTK) with potent whole blood activity and exceptional kinome selectivity. It exhibits potential efficacy in treatment for B-cell malignancies and autoimmune disorders. | ||
| E4597New | Avitinib maleate | Avitinib maleate(Abivertinib maleate, AC0010 maleate, AC0010MA) is a third-generation, irreversible, and orally active selective inhibitor of EGFR. It displays IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M, and wild-type EGFR. Avitinib maleate also acts as an inhibitor of BTK that induces apoptosis of BTK in mantle cell lymphoma. | ||
| E4643New | BIIB129 | BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS). | ||
| S9660 | Remibrutinib | Remibrutinib is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. | ||
| S8571 | BTK IN-1 | BTK IN-1(SNS062 analog) is a potent Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of <100 nM. | ||
| E0041 | Tolebrutinib | Tolebrutinib is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. | ||
| S6725 | PCI 29732 | PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. | ||
| E2201 | N-piperidine Ibrutinib hydrochloride | N-piperidine Ibrutinib hydrochloride, a reversible Ibrutinib derivative, is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. | ||
| S9600 | Orelabrutinib | Orelabrutinib is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity. | ||
| E1993New | BGB-16673 | BGB-16673(BTK-IN-29) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases. | ||
| E1625New | Elsubrutinib | Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus. | ||
| S8542 | Btk inhibitor 2 | Btk inhibitor 2 is a BTK inhibitor. | ||
| S9944 | PRN1008 | PRN1008 (Rilzabrutinib) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. | ||
| S2680 | Ibrutinib | イブルチニブ (Ibrutinib (PCI-32765)) は、無細胞アッセイで IC50 が 0.5 nM の強力で選択性の高い Brutons チロシンキナーゼ (Brutons tyrosine kinase, Btk) 阻害剤であり、Bmx, CSK, FGR, BRK, HCKに対しても阻害活性を持ちます。 EGFR, Yes, ErbB2, JAK3 に対しては前者より比較的弱い活性を持ちます。イブルチニブは、P13I を含む一連の PROTAC の合成における Btk リガンドとして適用できます。 |
|
|
| S8116 | Acalabrutinib (ACP-196) | Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR. |
|
|
| S7173 | Spebrutinib (AVL-292) | Spebrutinib (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1. |
|
|
| S8166 | tirabrutinib(ONO-4059) hydrochloride | Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. | ||
| S7051 | CGI1746 | CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
|
|
| S7734 | LFM-A13 | LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK. |
|
|
| S7257 | CNX-774 | CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
|
|
| S8294 | Olmutinib (BI 1482694) | Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase. | ||
| S8348 | BMS-935177 | BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. | ||
| S8421 | Fenebrutinib (GDC-0853) | Fenebrutinib (GDC-0853) is a potent, selective, and non-covalent bruton's tyrosine kinase (BTK) inhibitor with an Ki value of 0.91 nM for Btk with >100-fold selectivity over 3 off-targets (Bmx :153-fold, Fgr: 168-fold, Src:131-fold). | ||
| S8832 | Branebrutinib (BMS-986195) | Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. | ||
| S8741 | Avitinib (Abivertinib) | Avitinib (Abivertinib) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. | ||
| S8381 | BMS-986142 | BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX). | ||
| S8791 | Zanubrutinib | Zanubrutinib is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR. | ||
| S8711 | Nemtabrutinib (ARQ 531) | Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. | ||
| S9825 | Pirtobrutinib (LOXO-305) | Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases. | ||
| S7080 | RN486 | RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM. | ||
| S8679 | BTK inhibitor 1 (Compound 27) | BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. | ||
| E1381 | NX-2127 | NX-2127 is a unique, potent inhibitor of BTK that prevents its functions by catalyzing the ubiquitylation and proteasomal degradation of BTK rather than via direct binding. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells. | ||
| S7877 | ONO-4059 analogue | ONO-4059 analogue (ONO-WG-307) is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1. | ||
| E2838 | M7583 | M7583 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with IC50 and Ki of 1.5 nM and 11.9 nM, respectively. | ||
| E2843 | Poseltinib | Poseltinib (HM71224, LY3337641) shows a highly selective inhibition for Bruton’s tyrosine kinase (BTK) with IC50 of 1.95 nM, in which the selectivity toward other BMX, TEC and TXK are 0.3, 2.3 and 2.4 fold, respectively. | ||
| E1848New | BGB-8035 | BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. BGB-8035 exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases. | ||
| E1582New | Edralbrutinib | Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL). | ||
| E1611New | Atuzabrutinib | Atuzabrutinib (SAR 444727, PRN473) is a reversible, selective inhibitor of Bruton's tyrosine kinase (Btk). It can effectively prevent neutrophil recruitment via inhibition of macrophage antigen‐1 signalling. | ||
| S6966 | MT-802 | MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL). | ||
| E1355New | JNJ-64264681 | JNJ-64264681 is an orally active, irreversible covalent inhibitor of Bruton's tyrosine kinase (BTK) with potent whole blood activity and exceptional kinome selectivity. It exhibits potential efficacy in treatment for B-cell malignancies and autoimmune disorders. | ||
| E4597New | Avitinib maleate | Avitinib maleate(Abivertinib maleate, AC0010 maleate, AC0010MA) is a third-generation, irreversible, and orally active selective inhibitor of EGFR. It displays IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M, and wild-type EGFR. Avitinib maleate also acts as an inhibitor of BTK that induces apoptosis of BTK in mantle cell lymphoma. | ||
| E4643New | BIIB129 | BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS). | ||
| S9660 | Remibrutinib | Remibrutinib is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. | ||
| S8571 | BTK IN-1 | BTK IN-1(SNS062 analog) is a potent Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of <100 nM. | ||
| E0041 | Tolebrutinib | Tolebrutinib is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. | ||
| S6725 | PCI 29732 | PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. | ||
| E2201 | N-piperidine Ibrutinib hydrochloride | N-piperidine Ibrutinib hydrochloride, a reversible Ibrutinib derivative, is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. | ||
| S9600 | Orelabrutinib | Orelabrutinib is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity. | ||
| E1993New | BGB-16673 | BGB-16673(BTK-IN-29) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases. | ||
| E1625New | Elsubrutinib | Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus. | ||
| S8542 | Btk inhibitor 2 | Btk inhibitor 2 is a BTK inhibitor. | ||
| S9944 | PRN1008 | PRN1008 (Rilzabrutinib) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. | ||
| E1660New | NX-5948 | NX-5948(BTK-IN-24) is a novel oral small molecule that induces BTK degradation via cereblon E3 ubiquitin ligase recruitment. It mediates potent anti-inflammatory activity and can cross the blood-brain barrier in animal models. | ||
| E1848New | BGB-8035 | BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. BGB-8035 exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases. | ||
| E1582New | Edralbrutinib | Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL). | ||
| E1611New | Atuzabrutinib | Atuzabrutinib (SAR 444727, PRN473) is a reversible, selective inhibitor of Bruton's tyrosine kinase (Btk). It can effectively prevent neutrophil recruitment via inhibition of macrophage antigen‐1 signalling. | ||
| E1355New | JNJ-64264681 | JNJ-64264681 is an orally active, irreversible covalent inhibitor of Bruton's tyrosine kinase (BTK) with potent whole blood activity and exceptional kinome selectivity. It exhibits potential efficacy in treatment for B-cell malignancies and autoimmune disorders. | ||
| E4597New | Avitinib maleate | Avitinib maleate(Abivertinib maleate, AC0010 maleate, AC0010MA) is a third-generation, irreversible, and orally active selective inhibitor of EGFR. It displays IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M, and wild-type EGFR. Avitinib maleate also acts as an inhibitor of BTK that induces apoptosis of BTK in mantle cell lymphoma. | ||
| E4643New | BIIB129 | BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS). | ||
| E1993New | BGB-16673 | BGB-16673(BTK-IN-29) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases. | ||
| E1625New | Elsubrutinib | Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus. |
BTK阻害剤の選択性比較
BTKシグナル伝達経路
Tags: BTK inhibitor|BTK agonist|BTK activator|BTK inducer|BTK antagonist|BTK signaling pathway|BTK assay kit
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