Search Result
Results for "
imatinib
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15463
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Imatinib
Maximum Cited Publications
110 Publications Verification
STI571; CGP-57148B
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Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
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Cancer
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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 .
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- HY-G0017
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Norimatinib; imatinib metabolite N-Desmethyl imatinib
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Drug Metabolite
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Cancer
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N-Desmethyl imatinib (Norimatinib) is a c-Abl tyrosine kinase inhibitor. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways, and inhibits c-Abl-related neurodegenerative activity and neuroinflammation in vitro. N-Desmethyl imatinib can be used to study neurodegenerative diseases (such as Parkinson's disease) .
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- HY-15463S1
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STI571 d4; CGP-57148B d4
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Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
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Cancer
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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 .
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- HY-135638
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- HY-G0017S
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Norimatinib-d8; imatinib metabolite N-Desmethyl imatinib-d8
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Drug Metabolite
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Cancer
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N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib.
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- HY-131275
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Drug Metabolite
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Others
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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 .
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- HY-G0017A
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Norimatinib mesylate; imatinib metabolite N-Desmethyl imatinib mesylate
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Drug Metabolite
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Others
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N-Desmethyl imatinib mesylate (Norimatinib mesylate) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
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- HY-G0017S1
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Norimatinib-d4; imatinib metabolite N-Desmethyl imatinib-d4
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Isotope-Labeled Compounds
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Others
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N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
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- HY-50946R
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STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard)
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Reference Standards
c-Kit
Bcr-Abl
PDGFR
Autophagy
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Cancer
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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.
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- HY-G0017R
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Norimatinib (Standard); imatinib metabolite N-Desmethyl imatinib (Standard)
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Reference Standards
Drug Metabolite
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Others
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Clobutinol (hydrochloride) (Standard) is the analytical standard of Clobutinol (hydrochloride). This product is intended for research and analytical applications. Clobutinol hydrochloride is a compound that has anti-tussive effects. Clobutinol hydrochloride affects heart rate and blood pressure, it can be used for cough related research .
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- HY-15463R
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STI571 (Standard); CGP-57148B (Standard)
|
Reference Standards
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
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Cancer
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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 .
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- HY-132386S
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- HY-50946
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STI571 Mesylate; CGP-57148B Mesylate
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c-Kit
Bcr-Abl
PDGFR
Autophagy
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Cancer
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Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
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- HY-15463S2
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STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
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Autophagy
Bcr-Abl
c-Kit
SARS-CoV
PDGFR
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Cancer
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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.
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- HY-15463S
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STI571-d8; CGP-57148B-d8
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Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
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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 .
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- HY-111849
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CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding moiety 1
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Ligands for Target Protein for PROTAC
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Cancer
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Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
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- HY-15463S3
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STI571-13C,d3; CGP-57148B-13C,d3
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Isotope-Labeled Compounds
Autophagy
SARS-CoV
Bcr-Abl
PDGFR
c-Kit
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Cancer
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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 .
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- HY-131275R
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Drug Metabolite
Reference Standards
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Others
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Carglumic Acid (Standard) is the analytical standard of Carglumic Acid. This product is intended for research and analytical applications. Carglumic acid (N-Carbamyl-L-glutamic acid), a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
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- HY-146438
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PPAR
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Cancer
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PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
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- HY-146439
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PPAR
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Cancer
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PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
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- HY-157389
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Bcr-Abl
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Cancer
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AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-Abl T315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML) .
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- HY-150569
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Bcr-Abl
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Cancer
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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.
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- HY-111858
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SNIPERs
Bcr-Abl
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Cancer
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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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- HY-111851
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SNIPERs
Bcr-Abl
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Cancer
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SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM .
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- HY-E70639
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 Q252H Recombinant Human Active Protein Kinase is a recombinant ABL1 Q252H protein that can be used to study ABL1 Q252H-related functions .
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- HY-E70640
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 T315I Recombinant Human Active Protein Kinase is a recombinant ABL1 T315I protein that can be used to study ABL1 T315I-related functions .
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- HY-E70638
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 M351T Recombinant Human Active Protein Kinase is a recombinant ABL1 M351T protein that can be used to study ABL1 M351T-related functions .
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- HY-E70635
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 F317I Recombinant Human Active Protein Kinase is a recombinant ABL1 F317I protein that can be used to study ABL1 F317I-related functions .
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- HY-E70641
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 Y253F Recombinant Human Active Protein Kinase is a recombinant ABL1 Y253F protein that can be used to study ABL1 Y253F-related functions .
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- HY-E70636
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 G250E Recombinant Human Active Protein Kinase is a recombinant ABL1 G250E protein that can be used to study ABL1 G250E-related functions .
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- HY-E70637
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 H396P Recombinant Human Active Protein Kinase is a recombinant ABL1 H396P protein that can be used to study ABL1 H396P-related functions .
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- HY-E70634
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Bcr-Abl
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Cancer
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The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 E255K Recombinant Human Active Protein Kinase is a recombinant ABL1 E255K protein that can be used to study ABL1 E255K-related functions .
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- HY-111859
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SNIPERs
Bcr-Abl
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Cancer
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SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM .
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- HY-168730
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STAT
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Cancer
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Anticancer agent 259 (Compound 3g) is a Telmisartan (HY-13955)-based cell death modulator, that interfers with the STAT5 signaling pathway, enhances the sensitivity of drug-resistant cells to Imatinib (HY-15463) with SC50 of 1.5 μM .
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- HY-W143698
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Bcr-Abl
c-Kit
PDGFR
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Cancer
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PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
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- HY-156092
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BCRP
Apoptosis
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Cancer
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Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells .
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- HY-157327
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Bcr-Abl
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Cancer
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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 .
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- HY-125090
-
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Aurora Kinase
c-Myc
Bcr-Abl
Histone Methyltransferase
Apoptosis
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Cancer
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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 .
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- HY-101985
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-
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- HY-15666R
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GZD824 (Standard); HQP1351 (Standard)
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Reference Standards
Bcr-Abl
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Cancer
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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.
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- HY-15666A
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GZD824 dimesylate; HQP1351 dimesylate
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Bcr-Abl
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Cancer
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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.
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- HY-15666
-
GZD824; HQP1351
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Bcr-Abl
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Cancer
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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.
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- HY-164469
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Bcr-Abl
Apoptosis
STAT
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Cancer
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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) .
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- HY-112417
-
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PDGFR
FLT3
Apoptosis
Akt
PERK
Bcl-2 Family
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Cardiovascular Disease
Cancer
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Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis .
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- HY-164393
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JAK
Bcr-Abl
Apoptosis
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Cancer
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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 .
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Cat. No. |
Product Name |
Type |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15463S1
-
|
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 .
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-
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- HY-G0017S
-
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N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib.
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- HY-15463S2
-
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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.
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-
- HY-15463S
-
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 .
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- HY-G0017S1
-
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N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
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- HY-132386S
-
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Imatinib-d8 (mesylate) is the deuterium labeled Imatinib mesylate .
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- HY-15463S3
-
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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 .
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