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Results for "

BCR-ABL inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bcr-Abl (100) Ack1 (1) Akt (1) Antibiotic (1) Apoptosis (26) Aurora Kinase (3) Autophagy (26) Bacterial (1) Bcl-2 Family (1) c-Kit (14) c-Myc (1) Casein Kinase (1) CRISPR/Cas9 (1) Deubiquitinase (1) Drug Metabolite (6) FLT3 (3) HDAC (1) Histone Methyltransferase (1) IGF-1R (1) Isotope-Labeled Compounds (5) JAK (4) Microtubule/Tubulin (1) p38 MAPK (1) PDGFR (16) PROTACs (1) SARS-CoV (7) SNIPERs (12) Src (15) STAT (2) Thymidylate Synthase (1) Tyrosinase (1)
By Research Areas:	Cancer (105) Cardiovascular Disease (2) Endocrinology (1) Infection (1) Inflammation/Immunology (3) Neurological Disease (3)

By Targets:

Bcr-Abl (100)

Ack1 (1)

Akt (1)

Antibiotic (1)

Apoptosis (26)

Aurora Kinase (3)

Autophagy (26)

Bacterial (1)

Bcl-2 Family (1)

c-Kit (14)

c-Myc (1)

Casein Kinase (1)

CRISPR/Cas9 (1)

Deubiquitinase (1)

Drug Metabolite (6)

FLT3 (3)

HDAC (1)

Histone Methyltransferase (1)

IGF-1R (1)

Isotope-Labeled Compounds (5)

JAK (4)

Microtubule/Tubulin (1)

p38 MAPK (1)

PDGFR (16)

PROTACs (1)

SARS-CoV (7)

SNIPERs (12)

Src (15)

STAT (2)

Thymidylate Synthase (1)

Tyrosinase (1)

By Research Areas:

Cancer (105)

Cardiovascular Disease (2)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (3)

Neurological Disease (3)

111

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Bcr-Abl

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-157327

AKE-72	Bcr-Abl	Cancer
AKE-72 (compound 5) is a potent inhibitor of *Pan-BCR-ABL. AKE-72 inhibits* BCR-ABL ^WT, BCR-ABL ^T315, BCR-ABL ^E255K, BCR-ABL ^F3171, BCR-ABL ^H396P and BCR-ABL ^Q252H with IC₅₀s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line .

HY-142922

BCR-ABL-IN-4	Bcr-Abl	Cancer
BCR-ABL-IN-4 is a *BCR-ABL* inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC₅₀ values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .

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-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-161323

FLT3-ITD/D835Y-IN-1	FLT3 Bcr-Abl Apoptosis	Cancer
FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and *BCR-ABL* inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .

HY-136526

BCR-ABL-IN-3	Bcr-Abl	Cancer
BCR-ABL-IN-3 is a potent and irreversible *Bcr-Abl* inhibitor with an IC₅₀ of ≤100 nM for Ba/F₃Bcr-Abl ^T3151. BCR-ABL-IN-3 has anti-cancer activity .

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-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-172096

cSRC/BCR-ABL-IN-1	Bcr-Abl Src	Cancer
cSRC/BCR-ABL-IN-1 (compound 21b) is a potent *Bcr-Abl* and C-Src inhibitor with IC₅₀ values of 56.2, 101 nM for Bcr-Abl, C-Src, respectively. cSRC/BCR-ABL-IN-1 shows cytotoxicity activity .

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-10159A

Nilotinib monohydrochloride monohydrate 35+ 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-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-156148

BCR-ABL-IN-8	Bcr-Abl	Cancer
BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group .

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-11007

GNF-2 2 Publications Verification	Bcr-Abl SARS-CoV	Cancer
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of *Bcr-Abl. GNF-2 inhibits* Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

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-15666

Olverembatinib 5 Publications Verification GZD824; HQP1351	Bcr-Abl	Cancer
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-Abl ^T315I 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.

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-15666A

Olverembatinib dimesylate 5 Publications Verification GZD824 dimesylate; HQP1351 dimesylate	Bcr-Abl	Cancer
Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl ^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity . Olverembatinib (dimesylate) 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-169608

BCR-ABL-IN-11	Bcr-Abl	Cancer
BCR-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) .

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-15666R

Olverembatinib (Standard)	Bcr-Abl	Cancer
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-Abl ^T315I 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.

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-10181B

Dasatinib monohydrate Maximum Cited Publications 115 Publications Verification BMS-354825 monohydrate	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) monohydrate 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 monohydrate inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.

HY-10181A

Dasatinib hydrochloride Maximum Cited Publications 115 Publications Verification BMS-354825 hydrochloride	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) hydrochloride 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 hydrochloride inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.

HY-10181

Dasatinib Maximum Cited Publications 115 Publications Verification BMS-354825	Bcr-Abl Src Autophagy Apoptosis	Cancer
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-10159

Nilotinib 35+ Cited Publications AMN107	Bcr-Abl Autophagy	Cancer
Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

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-125780R

5-Phenylhydantoin (Standard)	Drug Metabolite	Cardiovascular Disease Neurological Disease
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate 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 monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.

HY-10181R

Dasatinib (Standard)	Bcr-Abl Src Autophagy Apoptosis	Cancer
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-10181BR

Dasatinib (monohydrate) (Standard)	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate 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 monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.

HY-15493

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

HY-10181S1

Dasatinib-d4 BMS-354825-d₄	Isotope-Labeled Compounds Autophagy Bcr-Abl Apoptosis Src	Cancer
Dasatinib-d₄ (BMS-354825-d₄) is deuterium labeled Dasatinib. 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-137460

Vodobatinib 1 Publications Verification 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-10181S

Dasatinib-d8 BMS-354825-d₈	Bcr-Abl Src Apoptosis Autophagy	Cancer
Dasatinib-d₈ is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

HY-13905

Flumatinib mesylate 2 Publications Verification HHGV678 mesylate	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of *Bcr-Abl. Flumatinib mesylate inhibits* c-Abl, PDGFRβ and c-Kit with IC₅₀ values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .

HY-125834

GMB-475	PROTACs Bcr-Abl Apoptosis STAT JAK	Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .

HY-10181G

Dasatinib (GMP) BMS-354825 (GMP)	Src Bcr-Abl Apoptosis Autophagy	Cancer
Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_i values for Src and *Bcr-Abl* are 16 pM and 30 pM, respectively. Dasatinib inhibits *Bcr-Abl* and Src with IC₅₀ values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy .

HY-50946

Imatinib Mesylate 95+ Cited Publications 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-111872

SNIPER(ABL)-020	SNIPERs Bcr-Abl	Cancer
SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of *BCR-ABL* protein .

HY-101489

GZD856	PDGFR Bcr-Abl Apoptosis	Cancer
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-10159S

Nilotinib-d6 AMN107-d₆	Bcr-Abl Autophagy	Cancer
Nilotinib-d₆ is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].

HY-111858

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

HY-132549S

Nilotinib-d3	Isotope-Labeled Compounds Bcr-Abl Autophagy	Cancer
Nilotinib-d₃ is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].

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.

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,280 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 1,280 compounds that act as a useful tool for PTKs-related drug screening and disease research.

HY-L129

Target Protein Ligand Library

56 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 56 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-108486

Herbimycin A	Infection Quinones Structural Classification Microorganisms Classification of Application Fields Source classification Benzene Quinones Disease Research Fields	Bacterial Antibiotic
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-125780R

5-Phenylhydantoin (Standard)	Microorganisms Source classification	Drug Metabolite
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate 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 monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.

Cat. No.	Product Name	Chemical Structure

HY-10181S

Dasatinib-d8
Dasatinib-d₈ is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

HY-10159S

Nilotinib-d6
Nilotinib-d₆ is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].

HY-132549S

Nilotinib-d3
Nilotinib-d₃ is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].

HY-15463S1

Imatinib-d4
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-15463S

Imatinib-d8 1 Publications Verification
Imatinib-d₈ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

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-10181S1

Dasatinib-d4

Dasatinib-d₄ (BMS-354825-d₄) is deuterium labeled Dasatinib. 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-10159S1

Nilotinib-13C,d3
Nilotinib-13C,d3 is a deuterated labeled Nilotinib . Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-13904S

Flumatinib-d3
Flumatinib-d₃ is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].

HY-15463S3

Imatinib-13C,d3

Imatinib- 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 .

HY-133794S

Dasatinib N-oxide-d8
Dasatinib N-oxide-d₈ is the deuterium labeled Dasatinib N-oxide. Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].

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