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Tyrosine Kinase

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Cat. No. Product Name Field of Application Chemical Structure
DC47979 HNMPA
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
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DC47915 RET-IN-7
RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
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DC47910 S116836
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor (TKI), blocks both wild-type as well as T315I Bcr-Abl. S116836 potently inhibits the phosphorylation of BCR-ABL and induces apoptosis. S116836 inhibits growth of WT and T315I mutant BCR-ABL tumors and does not cause significant cardiotoxicity. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies.
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DC47902 SH-1028 mesylate
SH-1028 (mesylate) is a selective and oral active inhibitor of EGFR with an IC50 of 18 nM. SH-1028 (mesylate) exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. SH-1028 (mesylate) significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
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DC47868 Zeteletinib hemiadipate
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.
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DC10641 PRN1371 Featured
PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.
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DC10996 DDR inhibitor X Featured
DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..
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DC45794 Tucatinib hemiethanolate Featured
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
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DC44827 Vodobatinib Featured
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.
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DC47324 Trk-IN-6
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).
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DC47657 LT-850-166
LT-850-166 is a potent FLT3 inhibitor with the capacity of overcoming a variety of FLT3 mutations.
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DC47592 ITK/TRKA-IN-1
ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
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DC47658 FGFR-IN-1
FGFR-IN-1 is a potent FGFR inhibitor with an IC50 of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219).
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DC47669 EGFR-IN-18
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
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DC47668 EGFR-IN-17
EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
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DC47667 EGFR/CSC-IN-1
EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer treatment.
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DC47679 Dyrk1A-IN-1
Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
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DC47719 BTK inhibitor 19
BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
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DC47331 AZ14145845
AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
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DC47332 Antiallergic agent-1
Antiallergic agent-1, a Src-family kinase inhibitor, may serve as a new valuable lead compound for future antiallergic drug discovery.
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DC47760 ALK-IN-13
ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19.
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DC47761 ALK-IN-12
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
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DC47314 TPX-0046
TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.,RET [1]() SRC [1]()
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DC47302 AZD8601
AZD8601 is an mRNA designed to produce vascular endothelial growth factor A (VEGF-A). AZD8601 accelerates diabetic wound healing.
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DC47279 Pegaptanib sodium
Pegaptanib sodium is an RNA aptamer directed against vascular endothelial growth factor (VEGF)-165. Pegaptanib could be used for the study of neovascular age-related macular degeneration (AMD) .
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DC47271 Tyrphostin 8
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
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DC47129 Zeteletinib
Zeteletinib (BOS-172738) shows selective inhibitory activity against RET, PDGFR, KIT, NTRK and FLT3 kinases. Zeteletinib has antitumor activity.
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DC47121 DDR2-IN-1
DDR2-IN-1 is potent DDR2 inhibitor with an IC50 of 26 nM. DDR2-IN-1, compound 129, can be used for osteoarthritis research.
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DC47115 Befotertinib
Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
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DC47018 Vepafestinib
Vepafestinib (compound 6) is a RET inhibitor (extracted from patent WO2019039439).
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