egfr tyrosine kinase

EGFR Protein Tyrosine Kinase Substrate is an EGFR protein tyrosine kinase substrate.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID:23528611 |Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID:22832269

Sacibertinib is a tyrosine kinase (Trk) inhibitor with activity against EGFR-TK phosphorylation (EC50: 110 nM) and HER2 (EC50: 244 nM), demonstrating antitumor effects.

Almonertinib mesylate is an irreversible inhibitor of EGFR tyrosine kinase with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate can be used in the non-small cell lung cancer studies.

VEGFR-IN-1 is a potent VEGFR2 inhibitor (IC50 = 3 nM). It blocks VEGF-induced signaling to suppress endothelial cell proliferation and angiogenesis in cancer research.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRβ, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature.

Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

GW 583340 dihydrochloride is a potent and orally available dual EGFR/ErbB2 (epidermal growth factor receptor/tyrosine kinase) inhibitor and is capable of reversing ABCG2- and ABCB1-mediated resistance.GW 583340 dihydrochloride selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, and inhibits 80% of tumor growth in a mouse xenograft model, with potential anticancer activity.

SU11652 is an effective and competitive receptor tyrosine kinase (RTK) inhibitor, including VEGFR, FGFR, PDGFR, and Kit. SU11652 disrupts the function of all forms of mutant Kit and may be used in the study of cancers involving Kit mutations.

Epitinib succinate (HMPL-813 succinate) is an orally active and brain penetration EGFR tyrosine kinase inhibitor and can be used in studies about cancer.

Zongertinib (BI 1810631) is a HER2 inhibitor, a selective HER2 tyrosine kinase inhibitor (with IC50 values of 13 nM and 579 nM for HER2 and EGFR, respectively), featuring covalent binding properties, used for solid tumor research.

EGFR-IN-87 is a potent EGFR tyrosine kinase inhibitor with anticancer activity that inhibits EGFR_d746-750, EGFR_L858R/T790M, and EGFR_WT in A431 cells, and can be used for cancer research.

BI-4732 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with high blood-brain barrier permeability, antitumor activity, inhibition of EGFR activation, and inhibition of T790M mutations.

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

ALK-IN-1 is a Brigatinib analog and an ALK inhibitor commonly used in anti-tumor research.

Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.