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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V10305 | Adaphostin | 241127-58-2 | Adaphostin(NSC-680410) is the adamantyl ester of AG957, acting as anovel and potent activator of Fas-mediated death pathwayin Bcr/Abl-positive leukaemia. |
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V3183 | Asciminib | 1492952-76-7 | Asciminib (formerly known as ABL-001; ABL001; trade name Scemblix) is a potent and selective allosteric inhibitor of BCR-ABL1 approved in Oct 2021 to treat Philadelphia chromosome-positive CML (chronic myeloid leukemia) with disease that meets certain criteria. |
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V6496 | Asciminib HCl | 2119669-71-3 | Asciminib HCl (ABL001; ABL-001; Scemblix), the hydrochloride salt ofAsciminib,is an allosteric inhibitor of BCR-ABL1 that has been approved FDA on Oct 29th 2021 for treating Philadelphia chromosome-positive CML (chronic myeloid leukemia). |
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V78599 | c-ABL-IN-5 | c-ABL-IN-5 is a selective c-Abl inhibitor (antagonist) with neuro-protection effects. | |
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V3720 | Dasatinib HCl | 854001-07-3 | Dasatinib (formerly known as BMS-354825; sold under the brand name Sprycel), is a novel, potent and multi-targeted, orally bioavailable synthetic small molecule inhibitor that targets Abl, Src and c-Kit, with IC50 of<1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
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V3405 | Flumatinib (HHGV-678) | 895519-90-1 | Flumatinib (HHGV-678; HHGV678; Hansoh Xinfu), the first approved 2nd generation TKI in China and an imatinib derivative, is a potent multi-kinase inhibitor with anticancer activity. |
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V3406 | Flumatinib mesylate (HHGV-678) | 895519-91-2 | Flumatinib mesylate (formerly HHGV678; HHGV-678), the mesylate salt of flumatinib which is first approved 2nd generation TKI in China and an imatinib derivative, is a potent inhibitor of multi-kinase such as c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM, respectively. |
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V28923 | Lyn-IN-1 | 887650-05-7 | Lyn-IN-1 (Bafetinib analogue),also known as INNO-406 analog and NS-187 analog, is a potent and selective dual Bcr-Abl/Lyn inhibitor, disclosed in patent WO2014169128A1. |
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V80789 | ML 2-23 | ML 2-23 is an effective PROTAC BCR-ABL degrader. | |
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V3387 | Olverembatinib (GZD824) | 1257628-77-5 | Olverembatinib (GZD824; HQP1351; trade name in China: Nailike) is an orally bioavailable, 3rd generation, and broad spectrum Bcr-Abl inhibitor that received approval in November 2021 in China for the treatment of adult patients with tyrosine kinase inhibitor (TKI)-resistant chronic phase chronic myeloid leukemia (CML-CP) or accelerated-phase CML (CML-AP) harboring the T315I mutation. |
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V3299 | Ponatinib HCl | 1114544-31-8 | Ponatinib HCl (AP-24534 HCl; Iclusig), the hydrochloride salt ofPonatinib, is an orally bioavailable and multi-targeted kinase inhibitor approved by the US FDA on December 14, 2012 for the treatment of resistant or intolerant CML and Ph+ ALL. |
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V76601 | PROTAC BCR-ABL Degrader-1 | PROTAC BCR-ABL Degrader-1 (Compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. | |
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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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