Bcr-Abl

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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 Related Products (151)
Recombinant Proteins (3)
Antibodies (6)

By Effects:	Inhibitors (136) Substrate (1) Degraders (4) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-15814

HG-7-85-01	Inhibitor	99.94%
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, VEGFR2/KDR/Flk-1 and RET with IC₅₀s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC₅₀>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.

HY-111872

SNIPER(ABL)-020	Inhibitor	99.79%
SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.

HY-101489A

GZD856 formic	Inhibitor	98.06%
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-Abl^T315I inhibitor, with IC₅₀s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-123450

S116836	Inhibitor	99.65%
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies. S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-P5426

Abl protein tyrosine kinase substrate	Substrate	98.96%
Abl protein tyrosine kinase substrate is a biological active peptide. (Abltide is a peptide substrate for Abl Kinase (Abl protein tyrosine kinase), a partner in the gag-Abl fusion protein of the Abelson murine leukemia virus. Used in Western blot and kinase assay.)

HY-123390

DB07107	Inhibitor
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC₅₀ value of 360 nM.

HY-15463S2

Imatinib-d₃ hydrochloride
Imatinib-d₃ (hydrochloride) is the deuterium 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.

HY-10158S

Bosutinib-d₈	Inhibitor	≥99.0%
Bosutinib-d₈ is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively[1][2].

HY-153008

BCR-ABL-IN-7	Inhibitor	≥98.0%
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research.

HY-12047S

Ponatinib-d₈	Inhibitor	99.91%
Ponatinib-d₈ is a deuterium labeled Ponatinib. Ponatinib (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/KDR/Flk-1, FGFR1, and Src, respectively.

HY-10181R

Dasatinib (Standard)	Inhibitor
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

HY-12338

ON 146040	Inhibitor
ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

HY-10159B

Nilotinib hydrochloride	Inhibitor
Nilotinib (AMN107) hydrochloride is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.

HY-101489

GZD856	Inhibitor
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-Abl^T315I inhibitor, with IC₅₀s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.

HY-119370

CHMFL-ABL-121	Inhibitor
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC₅₀s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.

HY-101034

CHMFL-ABL/KIT-155	Inhibitor
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC₅₀s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM) and PDGFRβ (IC₅₀=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.

HY-111871

SNIPER(ABL)-033	Inhibitor
SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC₅₀ of 0.3 μM (ABL inhibitor: HY-15814; ABL inhibitor activity control: HY-131178; E3 ligase ligand: HY-128808; linker: HY-130500; E3 ligase ligand + linker: HY-128819).

HY-108704

CT-721	Inhibitor
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC₅₀ of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities. CT-721 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-112314

AZD0424	Inhibitor
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.

HY-111858

SNIPER(ABL)-050	Inhibitor
SNIPER(ABL)-050, conjugating Imatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.

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Bcr-Abl

Bcr-Abl

Bcr-Abl Related Products (151)

Recombinant Proteins (3)

Antibodies (6)

Bcr-Abl Related Products (151):