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 potential antitumor activity.
AG957 (Tyrphostin AG-)957 is a novel and potent TKI-tyrosine kinase inhibitor, which selectively inhibits human p210 tyrosine kinase activity.
Ponatinib HCl (AP-24534 HCl; Iclusig), the hydrochloride salt of Ponatinib, 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.
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.
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.
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.
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.
Adaphostin (NSC-680410) is the adamantyl ester of AG957, acting as a novel and potent activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.
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.
Asciminib HCl (ABL001; ABL-001; Scemblix), the hydrochloride salt of Asciminib, 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).