Bcr-Abl
Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase.
Bcr-Abl Isoform Specific Products
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Bcr-Abl Inhibitors
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Bcr-Abl Antagonist
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Bcr-Abl Activator
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Bcr-Abl Modulators
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Bcr-Abl Degraders
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Bcr-Abl Substrate
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ABL1 Proteins
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Productos relacionados con Bcr-Abl (251)
Productos relacionados con (251)
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Recombinant Proteins (8)
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Antibodies (6)
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Bcr-Abl Isoform Comparison
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Dasatinib
0 ImagesSynonyms: BMS-354825Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier.
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Nocodazole
0 ImagesSynonyms: Oncodazole; R17934
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Imatinib
0 ImagesSynonyms: STI571; CGP-57148BImatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
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Bosutinib
0 ImagesSynonyms: SKI-606Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
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Puzerinostat mesylate
0 ImagesSynonyms: Purinostat mesylatePuzerinostat mesylate (Purinostat mesylate) is a highly selective class I/IIb histone deacetylase (HDAC) inhibitor, with IC50 values of 0.81 nM, 1.4 nM, 1.7 nM, 3.8 nM, 11.5 nM, and 1.1 nM against HDAC1, HDAC2, HDAC3, HDAC8, HDAC6, and HDAC10, respectively. Puzerinostat mesylate enhances glutamine metabolism by upregulating GLS1. Puzerinostat mesylate induces cell Apoptosis and downregulates the expression of BCR-ABL and c-MYC. Puzerinostat mesylate delays the progression of Ph+ B-cell acute lymphoblastic leukemia and prolongs the survival of relevant mouse models. Puzerinostat mesylate regulates the immune microenvironment. Puzerinostat mesylate can be used in research related to chronic myeloid leukemia, Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia, relapsed/refractory multiple myeloma, relapsed/refractory lymphoma, diffuse large B-cell lymphoma, and double-expression lymphoma.
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Puzerinostat
0 ImagesSynonyms: PurinostatPuzerinostat (Purinostat) is a highly selective class I/IIb histone deacetylase (HDAC) inhibitor, with IC50 values of 0.81 nM, 1.4 nM, 1.7 nM, 3.8 nM, 11.5 nM, and 1.1 nM against HDAC1, HDAC2, HDAC3, HDAC8, HDAC6, and HDAC10, respectively. Puzerinostat enhances glutamine metabolism by upregulating GLS1. Puzerinostat induces cell Apoptosis and downregulates the expression of BCR-ABL and c-MYC. Puzerinostat delays the progression of Ph+ B-cell acute lymphoblastic leukemia and prolongs the survival of relevant mouse models. Puzerinostat regulates the immune microenvironment. Puzerinostat can be used in research related to chronic myeloid leukemia, Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia, relapsed/refractory multiple myeloma, relapsed/refractory lymphoma, diffuse large B-cell lymphoma, and double-expression lymphoma.
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Asciminib
0 ImagesSynonyms: ABL001Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
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Degrasyn
0 ImagesSynonyms: WP1130Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
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Rebastinib
0 ImagesSynonyms: DCC-2036Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1WT and Abl1T315I, respectively. Rebastinib potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib inhibits the transcriptional activity of FoxO1. Rebastinib inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib induces Apoptosis. Rebastinib exerts anti-tumor activity in breast cancer. Rebastinib exerts anti-angiogenic effects. Rebastinib increases myotube diameter and improves reduced contractility. Rebastinib can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.
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Naporafenib
0 ImagesSynonyms: LXH254Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively.
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Olverembatinib
0 ImagesSynonyms: GZD824; HQP1351Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity. Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Dasatinib hydrochloride
0 ImagesSynonyms: BMS-354825 hydrochlorideDasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
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KW-2449
0 ImagesKW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
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Bafetinib
0 ImagesSynonyms: INNO-406; NS-187Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.
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Nilotinib monohydrochloride monohydrate
0 ImagesSynonyms: AMN107 monohydrochloride monohydrate
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GLPG3312
0 ImagesGLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
