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Bcr-Abl kinase inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bcr-Abl (43) Ack1 (1) Akt (1) Antibiotic (1) Apoptosis (8) Aurora Kinase (3) Autophagy (9) Bacterial (1) c-Kit (7) c-Myc (1) Casein Kinase (1) Drug Metabolite (3) FLT3 (1) Histone Methyltransferase (1) IGF-1R (1) JAK (3) p38 MAPK (1) PDGFR (7) SARS-CoV (2) Src (5) STAT (1) Thymidylate Synthase (1) Tyrosinase (1)
By Research Areas:	Cancer (45) Cardiovascular Disease (1) Endocrinology (1) Infection (1) Inflammation/Immunology (2) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Targets Recommended: Bcr-Abl

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15728

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

HY-10159A

Nilotinib monohydrochloride monohydrate 30+ Cited Publications AMN107 monohydrochloride monohydrate	Bcr-Abl Autophagy	Cancer
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against *BCR-ABL, and is active against many BCR-ABL* mutants.

HY-117718

AG957 Tyrphostin AG957; NSC 654705	Bcr-Abl	Cancer
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 p210 ^bcr/abl autokinase activity .

HY-150566

BCR-ABL-IN-5	Bcr-Abl	Cancer
BCR-ABL-IN-5 (compound II) is a **Bcr-Abl kinase** (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl ^WT and Bcr-Abl ^T3151 with the IC₅₀ value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .

HY-119177

PD173956	Bcr-Abl	Others
PD173956 is a pyridopyrimidine Bcr-Abl kinase inhibitor with high selectivity for the P-loop mutant form of Bcr-Abl .

HY-169230

BCR-ABL-IN-9	Bcr-Abl	Cancer
BCR-ABL-IN-9 (Compound B1) is a *BCR-ABL* inhibitor that achieves sustained *BCR-ABL* suppression by forming stable covalent bonds with the ABL kinase. BCR-ABL-IN-9 is also effective in inhibiting the activity of the ABL kinase (IC₅₀ = 1.2 nM). BCR-ABL-IN-9 possesses anticancer activity .

HY-150569

BCR-ABL-IN-6	Bcr-Abl	Cancer
BCR-ABL-IN-6 (9h) is a selective *Bcr-Abl* kinase inhibitor with IC₅₀s of 4.6 and 227 nM for Bcr-Abl ^WT and Bcr-Abl ^T3151 respectively. BCR-ABL-IN-6 inhibits *Bcr-Abl* kinase with strong affinity inside the cells with an EC₅₀ of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia . BCR-ABL-IN-6 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-160174

BCR-ABL kinase-IN-3	Bcr-Abl	Cancer
BCR-ABL kinase-IN-3 (example 1) is a potent inhibitor of *BCR-ABL* that plays an important role in acute myeloid leukemia (AML) research .

HY-160174A

BCR-ABL kinase-IN-3 (dihydrocholide)	Bcr-Abl	Cancer
BCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of *BCR-ABL* that plays an important role in acute myeloid leukemia (AML) research .

HY-169231

BCR-ABL-IN-10	Bcr-Abl	Cancer
BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing *BCR-ABL* inhibitor with an IC₅₀ of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML) .

HY-145887

BCR-ABL1-IN-1	Bcr-Abl	Neurological Disease
BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies .

HY-100314

BCR-ABL-IN-1	Bcr-Abl	Cancer
BCR-ABL-IN-1 is an inhibitor of *BCR-ABL* tyrosine kinase, with a pIC₅₀ of 6.46, and may be used in the research of chronic myelogenous leukemia.

HY-10159

Nilotinib 30+ Cited Publications AMN107	Bcr-Abl Autophagy	Cancer
Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-10159AR

Nilotinib monohydrochloride monohydrate (Standard)	Bcr-Abl Autophagy	Cancer
Nilotinib (monohydrochloride monohydrate) (Standard) is the analytical standard of Nilotinib (monohydrochloride monohydrate). This product is intended for research and analytical applications. Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against *BCR-ABL, and is active against many BCR-ABL* mutants.

HY-120036

Tyrphostin AG1112	Casein Kinase Tyrosinase	Cancer
Tyrphostin AG1112 is a potent inhibitors of CK II. Tyrphostin AG1112 inhibits p210 ^bcr-abl tyrosine kinase, with IC₅₀ values of 2, 15, 20 μM in p210 ^bcr-abl, EGFR and PDGFR cells, respectively .

HY-10943

GNF-7 2 Publications Verification	Bcr-Abl Ack1	Cancer
GNF-7 is a multikinase inhibitor. GNF-7 is a *Bcr-Abl* inhibitor, with IC₅₀s of 133 nM and 61 nM for Bcr-Abl ^WT and Bcr-Abl ^T315I, 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 .

HY-18819

BCR-ABL-IN-2	Bcr-Abl	Cancer
BCR-ABL-IN-2 is an inhibitor of *BCR-ABL1* tyrosine kinase, with IC₅₀s of 57 nM, 773 nm for ABL1 ^native and ABL1 ^T315I, respectively.

HY-15493

AN-019 NRC-AN-019	Bcr-Abl	Cancer
AN-019 is a *Bcr-Abl* kinase inhibitor. AN-019 has antitumor activity .

HY-50946

Imatinib Mesylate Maximum Cited Publications 85 Publications Verification STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, *Bcr-Abl, and PDGFR* (IC₅₀=100 nM) tyrosine kinases.

HY-108704

CT-721	Bcr-Abl	Cancer
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-103274

PD180970	Bcr-Abl Src c-Kit Apoptosis	Neurological Disease Cancer
PD180970 is a highly potent and ATP-competitive p210 ^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210 ^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .

HY-10159R

Nilotinib (Standard)	Bcr-Abl Autophagy	Cancer
Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-137460

Vodobatinib K0706	Bcr-Abl	Cancer
Vodobatinib (K0706) is a potent, third generation and orally active **Bcr-Abl1 tyrosine kinase** inhibitor with an IC₅₀ of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research . Vodobatinib 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-10159B

Nilotinib hydrochloride AMN107 hydrochloride	Bcr-Abl Autophagy	Cancer
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-50946R

Imatinib Mesylate (Standard) STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard)	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, *Bcr-Abl, and PDGFR* (IC₅₀=100 nM) tyrosine kinases.

HY-103032

Multi-kinase inhibitor 1	PDGFR c-Kit Bcr-Abl	Cancer
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* .

HY-15814

HG-7-85-01	Bcr-Abl PDGFR c-Kit Src JAK Apoptosis	Cancer
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, KDR 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-123390

DB07107	Bcr-Abl Akt	Cancer
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-131669

Dasatinib metabolite M6 Dasatinib carboxylic acid	Drug Metabolite	Others Cancer
Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib (HY-10181). Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor .

HY-15749

XL228 3 Publications Verification	Aurora Kinase Bcr-Abl IGF-1R Src	Endocrinology Cancer
XL228 is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 5, 3.1, 1.6, 6.1, 2 nM for *Bcr-Abl, Aurora A, IGF-1R, Src* and Lyn, respectively.

HY-101268

CHMFL-ABL-053	Bcr-Abl Src p38 MAPK	Cancer
CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available *BCR-ABL, SRC* and p38 kinase inhibitor with IC₅₀ values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively .

HY-160478

GNF-6	Bcr-Abl	Cancer
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of *BCR-ABL-T315I* with IC₅₀s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .

HY-107447

N-Deshydroxyethyl Dasatinib N-Deshydroxyethyl BMS-354825	Drug Metabolite	Inflammation/Immunology Cancer
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research .

HY-162952

cSRC/BCR-ABL1-IN-1	Bcr-Abl	Cancer
cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target *cSRC/BCR-ABL1* kinase inhibitor .

HY-153008

BCR-ABL-IN-7	Bcr-Abl	Cancer
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-126143

CHMFL-ABL-039	Bcr-Abl	Cancer
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant *BCR-ABL* inhibitor with the IC₅₀s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia .

HY-164469

CHMFL-48	Bcr-Abl Apoptosis STAT	Cancer
CHMFL-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) .

HY-108486

Herbimycin A	Bacterial Antibiotic	Infection
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 ^v-src and p210 ^BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.

HY-162489

Tyrosine kinase-IN-8	Bcr-Abl	Others
Tyrosine kinase-IN-8 (compound 4e) is a *BCR‐ABL1* tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC₅₀=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .

HY-15463

Imatinib Maximum Cited Publications 85 Publications Verification STI571; CGP-57148B	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
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-123450

S116836	Bcr-Abl Apoptosis PDGFR	Cancer
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-131275

Imatinib Impurity E	Drug Metabolite	Others
Imatinib Impurity E is the impurity of Imatinib. Imatinib 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-15463R

Imatinib (Standard)	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. 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-125090

PHA-680626	Aurora Kinase c-Myc Bcr-Abl Histone Methyltransferase Apoptosis	Cancer
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .

HY-147414

Vamotinib PF-114	Bcr-Abl	Cancer
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC₅₀s of 0.49 nM (ABL), 0.78 nM (ABL ^T315I), 9.5 nM (ABL ^E255K), 2.0 nM (ABL ^F317I), 7.4 nM (ABL ^G250E), 1.0 nM (ABL ^H396P), 2.8 nM (ABL ^M351T), 12 nM (ABL ^Q252H), and 4.1 nM (ABL ^Y253F), respectively . Vamotinib 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-162698

JMF4073	Thymidylate Synthase	Cancer
JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC₅₀s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo .

HY-118084

LS-104 Tyrene CR-4	JAK Bcr-Abl FLT3 Apoptosis	Cardiovascular Disease Inflammation/Immunology Cancer
LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, *Bcr-Abl* and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies .

HY-123159

AKI603	Aurora Kinase	Cancer
AKI603 is an inhibitor of *Aurora kinase* A (AurA), with an IC₅₀** of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .

HY-164393

ON044580	JAK Bcr-Abl Apoptosis	Cancer
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC₅₀s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 ^V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the *BCR-ABL* kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .

HY-50868

Bafetinib 5+ Cited Publications INNO-406; NS-187	Bcr-Abl Src Apoptosis	Cancer
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 .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,193 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,193 compounds that act as a useful tool for PTKs-related drug screening and disease research.

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