EphB Inhibitor
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EphB Inhibitor (5)
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JI-101
0 ImagesJI-101 is an orally active multi-kinase inhibitor. JI-101 inhibits EphB4, VEGFR-2 and PDGFR-β. JI-101 exhibits anticancer activity. JI-101 can be used in research related to ovarian cancer.
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EphB4-IN-1
0 ImagesCat. No.: HY-185227CAS No.: 1394837-94-5EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.
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PP124
0 ImagesCat. No.: HY-134468CAS No.: 1092788-95-8PP124 is a multi-kinase inhibitor. PP124 inhibits the phosphoinositide 3-kinase (PI3K) catalytic isoforms p110α, p110β, p110δ, and p110γ (IC50 = 4 μM, 7 μM, 0.966 μM, and 1.5 μM), mTOR and DNAPK (IC50 = 0.493 μM and 0.054 μM), as well as the tyrosine kinases Abl, Hck, Src, mutant Src (T/I), VEGFR, EGFR, and EphB4 (IC50 = 0.165 μM, 0.005 μM, 0.017 μM, 0.25 μM, 0.134 μM, 0.085 μM, and 0.17 μM). PP124 can be used for cancer research.
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JI-101 hydrochloride
0 ImagesCat. No.: HY-16265ACAS No.: 2514957-81-2JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity.JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis.JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes.JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
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EphB4-IN-2
0 ImagesCat. No.: HY-10654CAS No.: 1192216-03-7EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis.
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