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Bcr-Abl tyrosine kinase (Breakpoint cluster region Abelson) is a constitutively activated cytoplasmic tyrosine kinase (TK) and is the underlying cause of chronic myeloid leukemia (CML). To date, imatinib represents the frontline treatment for CML therapy. The development of resistance has prompted the search for novel Bcr-Abl inhibitors.

In Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL), the BCR-ABL translocation is the main transforming event; consequently, it is targeted by ABL-tyrosine kinase inhibitors (TKIs), the first of which to be identified was imatinib mesylate. There are now four newer TKIs, three so-called second-generation inhibitors and one third generation inhibitor, all of which are more potent than imatinib in in vitro assays. Since 2001, the Bcr-Abl inhibitor imatinib represents the first-line therapy for CML and also the second-generation Bcr-Abl inhibitor nilotinib and the dual BcrAbl/Src inhibitor dasatinib are now successfully used. Ponatinib, AP24534, by Ariad Pharmaceuticals Inc. has been approved by FDA for the treatment of resistant or imatinib-intolerant CML and Ph+ ALL patients, especially those harboring the T315I mutation. On September 2012, bosutinib received the approval by FDA and in 2013 it was approved also by European Medical Agency.

The search for Bcr-Abl inhibitors is very active. Bcr-Abl inhibitors constitute a very appealing research field that can be expected to expand further.



1. Soverini S, et al. Cancer. 2014 Apr 1;120(7):1002-9.

2. Thomas X, et al. Expert Opin Drug Discov. 2016 Nov;11(11):1061-1070.

3. Boer JM, et al. Eur J Cancer. 2017 Sep;82:203-218.

4. Shami PJ, et al. Leukemia. 2012 Feb;26(2):214-24.

5. Wylie AA,et al. Nature. 2017 Mar 30;543(7647):733-737.


Cat. No. Product Name Information


Bcr-Abl inhibitor

Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM).


BCR-ABL inhibitor

Flumatinib (HH-GV678) is a potent BCR-ABL/PDGFR/KIT inhibitor, potently inhibits ABL, PDGFR-β and KIT kinase with IC50 of 1.2, 307.6 and 665.5 nM, respectively.


BCR-ABL1 inhibitor

Vodobatinib (K0706) is a potent, selective inhibitor of BCR-ABL1 with IC50 of 7 nM (wt BCR-ABL1), exhibits activity against most clinically important BCR-ABL1 point mutants (M244V, IC50=22 nM).


Multikinase inhibitor

Olverembatinib (HQP1351, GZD824) is an orally bioavailable multikinase inhibitor targeting a broad spectrum of mutant KIT kinases (KIT-V559D IC50=1.4 nM).


BCR-ABL1 inhibitor

Radotinib (IY-5511) is a potent and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.


Bcr-Abl inhibitor

WP1130 (Degrasyn) is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression (IC50=1.8 uM), also inhibits deubiquitinases and blocks autophagy.


Bcr-Abl inhibitor

DCC-2036 (Rebastinib) is a highly potent, non-ATP-competitive BCR-ABL1 inhibitor with IC50 of 0.8 and 4 nM for native ABL1 and gatekeeper mutant ABL1 T315I, respectively.


Bcr-Abl inhibitor

Ponatinib (AP 24534) is a potent, orally active pan-inhibitor of BCR-ABL kinase with IC50 of 0.37 and 2.0 nM for ABL and mutant ABLT315I, respectively.


Bcr-Abl/Src/p38 inhibitor

CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM.


ABL1 inhibitor

Asciminib (ABL-001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR–ABL1-transformed BaF3 cells.


Multikinase inhibitor

CZC-8004 (CZC8004, Dianilinopyrimidine-01) is a pan-specific kinase inhibitor that binds to a broad range of tyrosine kinases, including ABL, BTK, FAK, FER, JAK1, SRC, SYK, TEC, TNK1, TYK2, and YES at low micromolar concentrations..

Imatinib mesylate

Imatinib mesylate (CGP-57148B, STI-571) is a n orally bioavailability mesylate salt of Imatinib, which is a multi-kinase inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 uM, 0.1 uM and 0.1 uM in cell-free or cell-based assays.

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