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Tyrosine Kinase

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Cat. No. Product Name Field of Application Chemical Structure
DC78269 Type II TRK inhibitor 3
Type II TRK inhibitor 3 (Compound 18d) is a Type II TRK inhibitor with IC50 values of 0.82, 1.82, and 0.12 nM for TRKAWT/G595R/G667C, respectively. Type II TRK inhibitor 3 exhibits antitumor activity.
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DC78237 AGW-11
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.
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DC78118 Enozertinib hemihydrate
Enozertinib (ORIC-114) hemihydrate is the inhibitor for EGFR that exhibits antineoplastic activity.
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DC78115 PF-06658607
PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry.
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DC78111 ISM7594
ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.
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DC78095 BMS-279700
BMS-279700 is an orally active Src-family kinase p56Lck inhibitor. BMS-279700 can block the production of proinflammatory cytokines (IL-2 and TNFα). BMS-279700 can inhibit T cell proliferation. BMS-279700 can be used for the researches of inflammation and immunology.
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DC78034 TCB-32
TCB-32 (Compound I-1) is a FGFR1 agonist with an EC50 of 0.88  μM. TCB-32 significantly increases cell proliferation through activating FGFR1 signaling pathway as bFGF and its downstream ERK 1/2 with excellent thermal stability. TCB-32 can replace bFGF in serum-free cell culture media. TCB-32 can be used for tissue repair and wound healing related diseases like psoriasis and eczema research.
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DC78021 (Rac)-Ibrutinib alkyne
(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC50 of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis.
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DC77995 Umedaptanib pegol
Umedaptanib pegol is an anti-fibroblast growth factor-2 (FGF2) aptamer. It is used for the study of neovascular age-related macular degeneration (nAMD).
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DC77994 Umedaptanib pegol sodium
Umedaptanib pegol sodium is an anti-fibroblast growth factor-2 (FGF2) aptamer. It is used for the study of neovascular age-related macular degeneration (nAMD).
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DC77966 Pegpleranib
Pegpleranib is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.
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DC77965 Pegpleranib sodium
Pegpleranib sodium is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.
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DC77921 IGFIIR aptamer sodium
IGFIIR aptamer sodium is an IGFIIR-specific aptamer that can be potentially used as a targeting ligand for the treatment and diagnosis of liver fibrosis.
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DC77917 MRC-G-001
MRC-G-001 is a Genipin derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.
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DC77876 Cibrigirsen
Cibrigirsen is an antisense oligonucleotide targeted to the insulin-like growth factor I receptor(IGF-1R).
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DC77875 Cibrigirsen sodium
Cibrigirsen sodium is an antisense oligonucleotide targeted to the insulin-like growth factor I receptor(IGF-1R).
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DC77872 CD117/c-Kit aptamer sodium
CD117/c-Kit aptamer sodium is a single-strand DNA aptamer specific for the biomarker CD117, which is highly expressed on acute myeloid leukemia (AML) cells.
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DC77853 ALN-3133 sodium
ALN-3133 sodium is a siRNA that targets VEGF, and it is one of the siRNAs in ALN-VSP.ALN-VSP is a lipid nanoparticle formulation containing two siRNAs for kinesin spindle protein (KSP) and VEGF with potential antitumor activity.
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DC77850 AGN-745
AGN-745 is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.
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DC77849 AGN-745 sodium
AGN-745 sodium is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.
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DC77828 BIEGi-1
BIEGi-1 is a potent and selective binary inhibitor of EGFR that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR–Rheb interaction. It robustly inhibits both EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. This compound exhibits significant anti-proliferative effects with an IC50 of 17 nM for PC9 and 20 nM for HCC827.
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DC40447 N-piperidine Ibrutinib hydrochloride Featured
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
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DC70547 KRCT-6j Featured
KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.
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DC70170 AC3573 Featured
AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.
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DC77201 Lenvatinib N-oxide
Lenvatinib N-Oxide (Lenvatinib impurity 10) is the impurity of Lenvatinib. DCG04 is a multivalent ligand for the mannose-6-phosphate receptor. DCG-04 is an activity-based probe for cysteine cathepsins, and can be used for labelling numerous cysteine cathepsins in cell and tissue lysates.
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DC77200 (Z)-SU14813
(Z)-SU14813 is an analog of SU14813. CAY10568 is physically smaller and less hydrophobic than the QX-314. CAY10568 can be used in studies of inflammation and pain perception.
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DC77199 VMD-928
VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma.
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DC77198 BNN27
BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable.
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DC77197 TG-100435
TG-100435 is a multitargeted, orally active protein tyrosine kinase inhibitor, with Ki of 13 to 64 nM for Src, Lyn, Abl, Yes, Lck, and EphB4. TG-100435 plays an important role in cancer research.
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DC77196 RK-20448
RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 derivative with neuroprotective and PP2A activating activities. FTY720-Mitoxy has the property of targeting mitochondria. In addition, FTY720-Mitoxy protects neurons by reducing inflammatory responses and is used in the study of neurodegenerative diseases such as Parkinson's disease.
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