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Protein Tyrosine Kinases
Catalog No. | Product Name | Application | Product Information |
---|---|---|---|
A10773 SALE |
RAF265 (CHIR-265) |
RAF/VEGFR Inhibitor |
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers.
|
A12357 SALE |
FIIN-2 |
FGFR Inhibitor |
FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
|
A13146 |
CL-387785 (EKI-785) |
EGFR inhibitor |
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
|
A16254 |
PD158780 |
EGFR inhibitor |
PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
|
A11263 |
BMS-690514 |
VEGFR/EGFR Inhibitor |
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.
|
A11558 SALE |
SU-5402 |
VVEGFR/FGFR/EGFR inhibitor |
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).
|
A12650 |
PKC 412 (Midostaurin) |
PKC inhibitor |
PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.
|
A13718 SALE |
Icotinib Hydrochloride |
EGFR inhibitor |
Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
|
A13681 SALE |
AZD-9291 (Osimertinib) |
EGFR inhibitor |
AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.
|
A13588 |
Tyrphostin AG 183 |
EGFR inhibitor |
Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM).
|
A13755 |
CNX-2006 |
EGFR inhibitor |
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
|
A13825 |
Icotinib |
EGFR inhibitor |
Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
|
A14985 |
Afatinib dimaleate |
EGFR inhibitor |
Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
|
A15081 |
Erlotinib mesylate |
EGFR inhibitor |
Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
|
A15093 |
Gefitinib hydrochloride |
EGFR Inhibitor |
Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
|
A15272 |
Vandetanib trifluoroacetate
|
VEGFR/EGFR inhibitor |
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
|
A15531 |
BIBX1382 |
EGFR inhibitor |
BIBX1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 _mu_M) and a range of other related tyrosine kinases (IC50 > 10 _mu_M),
|
A15509 |
WHI-P180 |
EGFR/Cdk2 inhibitor |
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
|
A15516 |
AZ5104 |
EGFR inhibitor |
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
|
A15551 |
AZD3759 |
EGFR inhibitor |
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR.
|
A14408 |
ASP8273 (Naquotinib) |
irreversible EGFR inhibitor |
ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
|
A14416 |
EGF816 (Nazartinib) |
EGFR T790M inhibitor |
EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.
|
A15940 |
AG-18 (Tyrphostin 23) |
EGFR Inhibitor |
AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431.
|
A15955 |
DM1-SMCC |
potent EGFR inhibitor |
DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate.
|
A10005 SALE |
(-)-Epigallocatechin gallate |
Antioxidant, antiangiogenic, antitumor agent |
(-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.
|
A10706 SALE |
Pelitinib (EKB-569) |
EGFR inhibitor |
Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
|
A10638 SALE |
Neratinib (HKI-272) |
HER2 inhibitor |
Neratinib (HKI-272) is a tyrosine kinase inhibitor.
|
A10211 SALE |
Canertinib (CI-1033) |
HER2/ErbB2 inhibitor |
Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).
|
A10141 SALE |
BIBW2992 (Afatinib) |
EGFR inhibitor |
BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.
|
A10116 SALE |
AZD8931 (Sapitinib) |
pan-EGFR/pan-erbB inhibitor |
AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.
|
A10991 |
WZ4002 |
EGFR Inhibitor |
WZ4002 is EGFR inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib.
|
A10422 SALE |
Gefitinib (Iressa) |
EGFR Inhibitor |
Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
|
A10362 SALE |
Erlotinib HCl |
EGFR inhibitor |
Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
|
A10514 SALE |
Lapatinib Ditosylate |
HER2 inhibitor |
Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
|
A11022 SALE |
AG-1478 (Tyrphostin AG-1478) |
EGFR Inhibitor |
AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
|
A10678 SALE |
OSI-420 |
EGFR Inhibitor |
OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .
|
A10992 |
WZ8040 |
EGFR Inhibitor |
WZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation.
|
A10990 |
WZ3146 |
EGFR Inhibitor |
WZ3146 is an inhibitor of EGFR receptor kinase mutants carrying a mutation in an active site gatekeeper residue (T790M) and is much less potent against wild-type EGFR kinase.
|
A10702 |
PD153035 (HCl salt) |
EGFR inhibitor |
PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR.
|
A10242 SALE |
CP-724714 |
HER2/ErbB2 inhibitor |
CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) .
|
A11209 SALE |
BMS 599626 (AC480) |
EGFR Inhibitor |
BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity.
|
A11027 |
Arry-380 analog |
HER2 Inhibitor |
ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.
|
A11028 |
AV-412 |
EGFR inhibitor |
AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.
|
A10047 SALE |
AG-490 |
EGFR inhibitor |
AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
|
A10043 SALE |
AEE788 |
EGFR inhibitor |
AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.
|
A10210 SALE |
Chrysophanic acid (Chrysophanol) |
EGFR inhibitor |
Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway.
|
A11051 SALE |
PF299804 (Dacomitinib, PF299) |
EGFR inhibitor |
PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.
|
A11057 |
XL647 (Tesevatinib) |
GFR, HER2 and VEGFR inhibitor |
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4.
|
A11155 SALE |
AST-1306 |
EGFR Inhibitor |
AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.
|
A10286 SALE |
Daphnetin |
EGFR, PKA,PKC inhibitor |
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 µM), PKA (IC50 = 9.33 µM), and PKC (IC50 = 25 µM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
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