Bcr-Abl
Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase.
Bcr-Abl Isoform Specific Products
All Product Categories
-
Bcr-Abl Inhibitors
(201)
View all products
-
Bcr-Abl Antagonist
(1)
View all products
-
Bcr-Abl Activator
(1)
View all products
-
Bcr-Abl Modulators
(2)
View all products
-
Bcr-Abl Degraders
(24)
View all products
-
Bcr-Abl Control
(1)
View all products
-
Bcr-Abl Substrate
(1)
View all products
-
ABL1 Proteins
(7)
View all products
-
Bcr-Abl Related Products (249)
Related Products (249)
-
Recombinant Proteins (7)
-
Antibodies (6)
-
Bcr-Abl Isoform Comparison
-
BCR-ABL kinase-IN-3
0 ImagesCat. No.: HY-160174CAS No.: 2699634-21-2
-
Olverembatinib (Standard)
0 ImagesSynonyms: GZD824 (Standard); HQP1351 (Standard)Olverembatinib (Standard) is the analytical standard of Olverembatinib. This product is intended for research and analytical applications. Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity. Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
-
CHMFL-48
0 ImagesCat. No.: HY-164469CAS No.: 2479290-65-6CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML).
-
Dasatinib hydrochloride (Standard)
0 ImagesSynonyms: BMS-354825 hydrochloride (Standard)Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
-
Bafetinib (Standard)
0 ImagesSynonyms: INNO-406 (Standard); NS-187 (Standard)Bafetinib (Standard) is the analytical standard of Bafetinib. This product is intended for research and analytical applications. Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.
-
GNF-7 (Standard)
0 ImagesCat. No.: HY-10943RCAS No.: 839706-07-9GNF-7 (Standard) is the analytical standard of GNF-7 (HY-10943). This product is intended for research and analytical applications. GNF-7 is a multiKinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 Kinase 1) and GCK (germinal center Kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
-
Asciminib hydrochloride (Standard)
0 ImagesSynonyms: ABL001 hydrochloride (Standard)Asciminib hydrochloride (Standard) is the analytical standard of Asciminib hydrochloride (HY-104010A). This product is intended for research and analytical applications. Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
-
Cenisertib benzoate
0 ImagesCat. No.: HY-13072BCAS No.: 1145859-64-8Synonyms: AS-703569 benzoate; R-763 benzoateCenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
-
Imatinib-13C,d3
0 ImagesCat. No.: HY-15463S3Synonyms: STI571-13C,d3; CGP-57148B-13C,d3Imatinib-13C,d3 (STI571-13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (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 also is an inhibitor of SARS-CoV and MERS-CoV.
-
AG957 (Standard)
0 ImagesCat. No.: HY-117718RCAS No.: 140674-76-6Synonyms: Tyrphostin AG957 (Standard); NSC 654705 (Standard)AG957 (Standard) is the analytical standard of AG957. This product is intended for research and analytical applications. AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity.
-
Multi-kinase-IN-11
0 ImagesCat. No.: HY-18909CAS No.: 1157857-36-7
-
Nilotinib-d3
0 ImagesCat. No.: HY-132549SCAS No.: 1215678-43-5Nilotinib-d3 is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
-
Adaphostin (Standard)
0 ImagesSynonyms: NSC 680410 (Standard)Adaphostin (Standard) is the analytical standard of Adaphostin. This product is intended for research and analytical applications. Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells.
-
KW-2449 (Standard)
0 ImagesCat. No.: HY-10339RCAS No.: 1000669-72-6
-
HS-438
0 ImagesCat. No.: HY-123486CAS No.: 1430720-10-7HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML).
-
Multi-kinase inhibitor 1 (Standard)
0 ImagesCat. No.: HY-103032RCAS No.: 778274-97-8Multi-kinase inhibitor 1 (Standard) is the analytical standard of Multi-kinase inhibitor 1 (HY-103032). This product is intended for research and analytical applications. Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
-
BCR-ABL-IN-11
0 ImagesBCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor. BCR-ABL-IN-11 shows anticancer activity against chronic myelogenous leukemia (CML) (IC50 of 129.61 μM for K562 cells).
-
AFG210
0 ImagesCat. No.: HY-18817CAS No.: 228400-22-4AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.
-
Enzyme modulator-1
0 ImagesCat. No.: HY-186223CAS No.: 897375-76-7
