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.

Rebastinib (formerly also known as DCC-2036), a novel, potent and orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity, is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50s of 0.8 nM and 4 nM. It also inhibits other kinases such as SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, […]

Olverembatinib Dimesylate (GZD-824; HQP-1351; trade name in China: Nailike), the dimesylate salt of GZD824 (HQP1351), is a novel, potent, orally bioavailable Bcr-Abl inhibitor with potential antineoplastic activity. As of November 2021, Olverembatinib has been approved in China for the treatment of adult patients with tyrosine kinase inhibitor (TKI)-resistant chronic phase chronic myeloid leukemia (CML-CP) or […]

Nilotinib (formerly also known as AMN-107, AMN107; trade name Tasigna) is a potent, orally bioavailable aminopyrimidine-based Bcr-Abl inhibitor with antineoplastic activity. It inhibits Bcr-Abl with an IC50 of<30 nM in Murine myeloid progenitor cells. As of 2007, nilotinib was approved by the US FDA for the treatment of imatinib-resistant chronic myelogenous leukemia which has the […]

GNF-5 (GNF 5; GNF5), a GNF-2 analog with better pharmacokinetic profiles, is a potent, selective and allosteric/non-ATP competitive Bcr-Abl inhibitor with potential anticancer activity. It inhibits Bcr-Abl (wild-type Abl) with an IC50 of 220 nM. It exhibits excellent in vivo anticancer efficacy in Ba/F3.p210 xenograft mouse model.

GNF-2 (GNF 2; GNF2) is a highly potent, selective and allosteric/non-ATP competitive inhibitor of Bcr-Abl with potential anticancer activity. It shows no activity against Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. GNF-2 acts by allosterically binding the myristate-binding site of ABL and inhibits the proliferation of BCR-ABL positive cell and induces cell apoptosis. GNF-2 […]

Degrasyn (formerly also known as WP1130) is a novel, potent, and selective small molecule inhibitor of deubiquitinases (DUBs such as USP5, USP14, USP9x, UCH-L1, and UCH37). It also suppresses Bcr/Abl, also a JAK2 transducer without affecting 20S proteasome and an activator of transcription (STAT). It exhibits excellent in vivo antitumor efficacy in Swiss Nu/Nu mice […]

GNF-7 (GNF7; GNF 7) is a novel, potent, orally bioactive/bioavailable Bcr-Abl kinase inhibitor with potential anticancer activity. It inhibits the following kinases: M351T, T315I, E255 V, G250E and c-Abl, with IC50s of<5 nM, 61 nM, 122 nM, 136 nM, and 133 nM, respectively. It demonstrate significant in vivo antitumor efficacy in SCID beige female mice […]

Radotinib (formerly IY-5511; IY5511; trade name Supect) is a novel, potent, selective, orally bioavailable, and 2nd generation BCR-ABL1 tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits BCR-ABL1 with an IC50 of 34 nM. It was developed by Ilyang Pharmaceutical in S. Korea and has the potential for the treatment of Chronic Myeloid Leukemia.

Bafetinib (formerly INNO406; NS-187), an investigational anticancer drug originally developed by Nippon Shinyaku and later licensed to CytRx, is an orally bioavailable dual Bcr-Abl/Lyn inhibitor with potential antineoplastic activity. It inhibits Bcr-Abl/Lyn with IC50s of 5.8 nM/19 nM in cell-free assays. In Bcr-Abl–positive KU812 mouse model, Bafetinib significantly inhibited tumor growth, and completely inhibited tumor […]