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-20215	PF-114 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).
PC-20144	IkT-148009 c-Abl inhibitor	IkT-148009 (Risvodetinib, 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-38393	Flumbatinib 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.
PC-38379	Vodobatinib 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).
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-38306	Olverembatinib 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).
PC-38025	Radotinib 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.
PC-43444	WP1130 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.
PC-43334	DCC-2036 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.
PC-42862	Ponatinib 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.
PC-63026	CHMFL-ABL-053 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.

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