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Bcr-Abl

Bcr-Abl

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.

Bcr-Abl related products

Structure Cat No. Product Name CAS No. Product Description
Adaphostin 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.
AK-HW-90 V84226 AK-HW-90
AKE-72 V85947 AKE-72 2566525-18-4
Asciminib 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.
Asciminib HCl 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).
BCR-ABL kinase-IN-3 V85499 BCR-ABL kinase-IN-3 2699634-21-2
BCR-ABL kinase-IN-3 (dihydrocholide) V85510 BCR-ABL kinase-IN-3 (dihydrocholide)
c-ABL-IN-5 V78599 c-ABL-IN-5 c-ABL-IN-5 is a selective c-Abl inhibitor (antagonist) with neuro-protection effects.
c-ABL-IN-6 V84924 c-ABL-IN-6
DA5-HTL V85041 DA5-HTL
Dasatinib HCl 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.
Flumatinib (HHGV-678) 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.
Flumatinib mesylate (HHGV-678) 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.
GNF-6 V83693 GNF-6 839708-29-1
HG-7-86-01 V85409 HG-7-86-01 1258391-14-8
Lyn-IN-1 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.
ML 2-23 V80789 ML 2-23 ML 2-23 is an effective PROTAC BCR-ABL degrader.
Olverembatinib (GZD824) 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.
Ponatinib HCl 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.
PROTAC BCR-ABL Degrader-1 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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