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Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13/4.2/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 = 2 μM), ErbB2 (IC50 = 13.5 μM), STAT3 and JAK2.
Pazopanib HCl is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.
5-Iodotubercidin is a potent inhibitor (IC50 = 26 nM). It also inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
Afatinib E-isomer is an irreversible inhibitor of dual EGFR and HER2 that shows obvious activitives of EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM respectively.
GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.
Necrosulfonamide is a necroptosis inhibitor by blocking mixed lineage kinase domain-like protein (MLKL), a key substrate of receptor-interacting serine-threonine kinase 3 (RIP3).
Imatinib Mesylate is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.
PD153035 HCl is an reversible inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
Piceatannol, a natural stilbene, is selective Syk inhibitor extracted from the rhizomes of Polygonum cuspidatum Sieb. et Zucc..
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM.
TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM.
Tyrphostin RG14620 is an EGFR inhibitor of tyrphostin family, which selectively reverses ABCG2-mediated multidrug resistance in cancer cell lines.
Mubritinib is a potent and selective inhibitor of HER2/ErbB2 with IC50 of 6 nM with no inhibition on EGFR, FGFR, PDGFR, and etc.
Pelitinib irreversiblly inhibits EGFR with IC50 of 38.5 nM.
AG-18 is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 35 μM.
Staurosporine is a prototypical potent ATP-competitive multikinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.
Methyl 2,5-dihydroxycinnamate, the erbstatin analog, is an inhibitor of EGF receptor-associated tyrosine kinases.
RG-13022 significantly inhibited EGF-stimulated autophosphorylation of its receptor in two breast cancer cell lines that have abundant, although not amplified, EGF receptor content (MDA-231 and T47D).RG-13022 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice. RG-13022 also increased the life span of these tumor-bearing nude mice.
Tags: 酪氨酸 | Tyrosine / EGF Receptor Protein Kinase Inhibitor | 酶抑制剂 | Enzyme Inhibitor | 酪氨酸 相关产品
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