Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML).A chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome is the root cause of more than 90% of CML cases. This abnormality results from the fusion of the break point cluster (Bcr) gene at chromosome 22 with the Abelson (Abl) tyrosine kinase gene at chromosome 9, creating a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been linked to the pathogenesis of CML. The tyrosine kinase has been selectively inhibited by substances.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V81390 | SIAIS100 | SIAIS100 is a potent BCR-ABL PROTAC degrader with DC50 of 2.7 nM. | |
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V81408 | SNIPER(ABL)-013 | SNIPER(ABL)-013, which is made up of GNF5 (ABL inhibitor) and Bestatin (IAP ligand) through a linker, can effectively degrade BCR-ABL protein with DC50 of 20 μM. | |
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V81409 | SNIPER(ABL)-015 | SNIPER(ABL)-015, which is made up of GNF5 (ABL inhibitor) and MV-1 (IAP ligand) through a linker, can effectively degrade BCR-ABL protein with DC50 of 5μM. | |
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V81410 | SNIPER(ABL)-019 | SNIPER(ABL)-019, which is made up of Dasatinib (ABL inhibitor) and MV-1 (cIAP1 ligand) through a linker, can effectively degrade BCR-ABL protein with DC50 of 0.3 μM. | |
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V76499 | SNIPER(ABL)-020 | SNIPER(ABL)-020, which is composed of Dasatinib (ABL inhibitor) and Bestatin (IAP ligand) through a linker, can effectively degrade BCR-ABL protein. | |
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V81411 | SNIPER(ABL)-044 | SNIPER(ABL)-044, which is made up of HG-7-85-01 (ABL inhibitor) and Bestatin (IAP ligand) through a linker, can effectively degrade BCR-ABL protein with DC50 of 10 μM. | |
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V81412 | SNIPER(ABL)-047 | SNIPER(ABL)-047, which is made up of HG-7-85-01 (ABL inhibitor) and MV-1 (IAP ligand) through a linker, can effectively degrade BCR-ABL protein with DC50 of 2 μM. | |
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V81413 | SNIPER(ABL)-049 | SNIPER(ABL)-049, which is made up of Imatinib (ABL inhibitor) and Bestatin (IAP ligand) through a linker, can effectively degrade BCR-ABL protein, with DC50 of 100 μM. | |
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V81414 | SNIPER(ABL)-050 | SNIPER(ABL)-050, which is composed of Imatinib (ABL inhibitor) and MV-1 (IAP ligand) through a linker, can effectively degrade BCR-ABL protein. | |
|
V10992 | Tyrphostin AG 957 | 140674-76-6 | AG957 (Tyrphostin AG957; NSC 654705) is a tyrosine kinase inhibitor (TKI) (antagonist) with anti-BCR/ABL tyrosine kinase activity. |
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