| Cat.No. | Name | Information |
|---|---|---|
| M3517 | Lapatinib | Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively. |
| M1802 | Lapatinib ditosylate monohydrate | Lapatinib (GW572016) ditosylate monohydrate is a selective and effective inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase (Ki = 347 nM). |
| M1749 | Gefitinib | Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages. |
| M5621 | Erlotinib (CP-358774) | Erlotinib (CP-358774) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. |
| M1913 | Neratinib | Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase. |
| M1850 | WZ4002 | WZ4002 is a novel, selective EGFR kinase inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) with IC50 of 8 nM. |
| M1869 | Dacomitinib | Dacomitinib (PF-00299804) is an oral, irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases. |
| M5307 | Afatinib dimaleate | Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. |
| M2424 | AZD9291 (Osimertinib) | Osimertinib (AZD-9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. |
| M1677 | Afatinib | Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. |
| M14134 | Rociletinib hydrobromide | Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. |
| M14133 | BMS-599626 Hydrochloride | BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. |
| M14131 | AV-412 free base | AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. |
| M11448 | BLU-945 | Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. |
| M11447 | Sunvozertinib | Sunvozertinib (DZD9008) is an effective inhibitor of ErbBs (EGFR, Her2, especially mutants) and BTK. |
| M11417 | (S)-Sunvozertinib | (S)-Sunvozertinib ((S)-DZD9008) is the S-enantiomer of Sunvozertinib, EGFR exon 20 NPH and ASV insertion, EGFR L858R/T790M mutation and Her2 exon 20 YVMA insertion (IC50 was 51.2 nM, 51.9 nM, 1 nM and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK. |
| M11415 | (Rac)-JBJ-04-125-02 | (Rac)-JBJ-04-125-02 is a racemate of JBJ-04-125-02, which is a potent, selectively mutated, allosteric and oral active EGFR inhibitor. The IC50 of EGFRL858R/T790M was 0.26 nM. |
| M10709 | TAS0728 | TAS0728 is an effective, selective, oral, irreversible, covalently bound HER2 inhibitor covalently bound to the C805 site of HER2, inhibiting its activity.IC50 The value is 13 nM. TAS0728 to BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and HUMAN HER2 IC50 The values are 4.9, 8.5, 31, 65, 33, 25, 86, and 36 nM, respectively. TAS0728 simultaneously inhibits phosphorylation of HER2, HER3 and its downstream effector proteins. Has antitumor activity. |
| M10509 | TX1-85-1 | TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. |
| M10472 | AZD3759 hydrochloride | AZD3759 (Zorifertinib) hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. |
| M10337 | Avitinib (AC0010) | Avitinib (Abivertinib; AC0010) is a third-generation irreversible EGFR tyrosine kinase inhibitor, with potential antineoplastic activity. |
| M10038 | Tucatinib | Tucatinib, also known as Irbinitinib and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (HER2). |
| M9938 | Lazertinib | Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR. |
| M9722 | Tyrphostin AG528 | Tyrphostin AG528 (Tyrphostin B66) is an inhibitor of EGFR and ErbB2 with IC50 values of 4.9 and 2.1 μM, respectively. |
| M9711 | AG1557 | AG1557 is a potent and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with pIC50 value of 8.194. |
| M9709 | NSC228155 | NSC228155 is an activator of EGFR, which binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. |
| M9686 | Tarloxotinib bromide | Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor. |
| M9642 | EGFR inhibitor 324674 | EGFR inhibitor 324674 is a cell permeable, potent and selective EGFR inhibitor with IC50 of 21 nM. |
| M9535 | Mobocertinib | Mobocertinib (TAK-788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. |
| M9534 | TAS6417 | TAS6417 is a novel EGFR inhibitor targeting exon 20 insertion mutations, with IC50 values range from 1.1-8.0 nM. |
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