Bcr-Abl (inhibitors, antagonists, agonists)-ProbeChem.com

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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.

References:

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
PC-45880	Bafetinib Abl/Lyn inhibitor	Bafetinib (INNO-406, NS-187) is a potent and selective dual Abl/Lyn tyrosine kinase inhibitor with IC50 of 5.9 nM and 198 nM, respectively.
PC-20144	IkT-148009 c-Abl inhibitor	IkT-148009 (IkT09) is a potent, selective, orally bioavailable and brain-penetrant c-Abl inhibitor with IC50 of 33 and 14 nM for c-Abl (Abl1) and its closely related isoform c-Abl2 (Arg), respectively.
PC-38592	Adaphostin Bcr-Abl inhibitor	Adaphostin (AG 957 Adamantyl Ester, NSC 680410) is a p210 Bcr/Abl tyrosine kinase inhibitor with IC50 of 14 uM, induces apoptosis in T-lymphoblastic human leukemia cell lines with IC50 of 16.8-216.3 nM.
PC-73114	PD180970 p210 bcr/abl inhibitor	PD180970 (PD 180970) is an ATP-competitive inhibitor of p210bcr/abl tyrosine kinase, inhibits autophosphorylation of p210Bcr-Abl with IC50 of 5 nM.
PC-43334	DCC-2036	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.
PC-42862	Ponatinib	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.
PC-42854	Lyn-IN-1	Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor..
PC-63026	CHMFL-ABL-053	CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM.
PC-62850	ABL-IN-29	ABL-IN-29 is a picomolar ABL kinase inhibitor with IC50 of 0.06/0.11 nM for wt ABL and ABL T315I respectively..
PC-42408	Nilotinib monohydrochloride monohydrate	A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.
PC-42427	Dasatinib hydrochloride	A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.
PC-42783	GNF-2	A potent, allosteric, non-ATP competitive Bcr-Abl inhibitor that shows exclusive antiproliferative activity toward Bcr-abl-transformed cells.

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