Bcr-Abl

Bcr-Abl inhibitor

Imatinib Mesylate (STI571) is an orally bioavailable multi-target inhibitor with IC 50 values for Bcr-Abl, c-Kit and PDGFR are 0.6μM, 0.1μM and 0.1μM respectively.

Src family kinases inhibitor

P210bcr/abl tyrosine kinase inhibitor

Abl kinases inhibitor

Bosutinib (SKI-606) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.

Dual Src/Abl kinase inhibitor, ATP-competitive,

DCC-2036 (Rebastinib) (DCC-2036) is an orally active, non-ATP-competitiveBcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. DCC-2036 (Rebastinib) also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.

Ponatinib (AP24534) (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

Bcr-Abl inhibitor

Saracatinib (AZD0530) (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib (AZD0530) shows high selectivity over other tyrosine kinases.

P210bcr/abl tyrosine kinase inhibitor

Imatinib (STI571) (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib (STI571) also is an inhibitor of SARS-CoV and MERS-CoV.

Type II Bcr-Abl inhibitor

Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity.

WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.

Bcr-Abl tyrosine kinase inhibitor

PDGRFβ inhibitor

Nocodazole is an anti-mitotic drug and a rapid and reversible microtubule polymerization inhibitor. It inhibits Abl, Abl (E255K), and Abl (T315I) in cell-free assays with IC 50 values of 0.21μM, 0.53μM, and 0.64μM, respectively.

Inhibitor of ABL, SRC, KIT, PDGFR, and other tyrosine kinases.

Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

Asciminib (ABL001) (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.

Flumatinib (HHGV678) (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib (HHGV678) inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.

GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.