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 |
---|---|---|---|---|
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. | |
V84226 | AK-HW-90 | |||
V85947 | AKE-72 | 2566525-18-4 | ||
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. | |
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). | |
V85499 | BCR-ABL kinase-IN-3 | 2699634-21-2 | ||
V85510 | BCR-ABL kinase-IN-3 (dihydrocholide) | |||
V78599 | c-ABL-IN-5 | c-ABL-IN-5 is a selective c-Abl inhibitor (antagonist) with neuro-protection effects. | ||
V84924 | c-ABL-IN-6 | |||
V85041 | DA5-HTL | |||
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. | |
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. | |
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. | |
V83693 | GNF-6 | 839708-29-1 | ||
V85409 | HG-7-86-01 | 1258391-14-8 | ||
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. | |
V80789 | ML 2-23 | ML 2-23 is an effective PROTAC BCR-ABL degrader. | ||
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. | |
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. | |
V76601 | PROTAC BCR-ABL Degrader-1 | PROTAC BCR-ABL Degrader-1 (Compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. |