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Erbb2 (HER2) belongs to Erbb family lacks the capacity to interact with a ligand because its extracellular region exists in a fixed, unfolded conformation. Erbb2 (HER2) acts as an amplifier of the Erbb signaling network. The adaptors and effector of Erbb2 includes Shc, Syk, RasGAP, Grb2/7, Abl, Mapk8, PLC and STAT1/3. Erbb3 lacks kinase activity and can form heterodimeric complexes with Erbb2. The ERBB2–ERBB3 dimer can be an important cancer therapeutic target.
| Cat.No. | Product Name | Information | Publication | Customer Review |
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| S1011 | Afatinib (BIBW2992) | BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively. |
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| S1167 | CP-724714 | CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM and also inhibits EGFR with IC50 of 6.4 μM. |
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(2)
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| S2216 | Mubritinib (TAK 165) | Mubritinib (TAK 165) is a potent inhibitor of ErbB2 with IC50 of 6 nM. |
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| S1019 | CI-1033 (Canertinib) | CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively. |
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| S1194 | CUDC-101 | CUDC-101 is a potent multi-target inhibitor targeting HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, respectively. |
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(2)
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| S2150 | Neratinib (HKI-272) | Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively. |
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| S2192 | AZD8931 | AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, respectively. |
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| S2816 | Tyrphostin AG 879 (AG 879) | AG879 inhibits both ErbB2 and Flk-1 with IC50 of 1 μM. |
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| S2784 | TAK-285 | TAK-285 is a novel dual HER2 and EGFR inhibitor with IC50 of 17 nM and 23 nM, respectively. |
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| S2752 | Arry-380 | ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM and also inhibits EGFR with IC50 of 4 μM. |
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| S2733 | AV-412 | AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor. |
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