EGFR/HER2

Items 401-450 of 493

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  1. EGFR inhibitor

    Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
  2. EGFR/T790M inhibitor

    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
  3. HER1/HER2 inhibitor

    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively.
  4. EGFR inhibitor

    AST2818 mesylate is an EGFR inhibitor.
  5. EGFR inhibitor

    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
  6. EGFR inhibitor

    Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
  7. EGFR/HER2 dual inhibitor

    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.
  8. EGFR, HER2 and HER4 inhibitor

    Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  9. EGFR inhibitor

    BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFR.
  10. FGFR-1, PDGFR-β, EGFR inhibitor

    PD089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR with IC50 of 0.15 µM, 1.76 µM, and 5.47 µM, respectively.

  11. EGFR inhibitor

    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
  12. EGFR inhibitor

    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM.
  13. EGFR inhibitor

    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations.
  14. EGFR/HER2 oncogenic mutants inhibitor

    Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  15. EGFR tyrosine kinase inhibitor

    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.
  16. Anticancer agent

    BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  17. EGFR inhibitor

    Alflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.
  18. EGFR inhibitor

    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
  19. FLK-1 (VEGFR-2) / HER2 inhibitor

    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
  20. EGFT/HER2 inhibitor

    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  21. VEGFR2 and EGFR signalling inhibitor

    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  22. EGFR inhibitor

    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae).
  23. dual inhibitor for c-Met and EGFR

    Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
  24. EGFR inhibitor

    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  25. T790M-Containing EGFR Mutants inhibitor

    PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants.
  26. EGFR antagonist

    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
  27. EGFR inhibitor

    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  28. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  29. Raf/EGFR inhibitor

    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
  30. EGFR inhibitor

    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
  31. EGFR/HER2/HER4 inhibitor

    BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
  32. EGFR inhibitor

    TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
  33. EGFR inhibitor

    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
  34. tyrosine kinase inhibitor

    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
  35. EGFR inhibitor

    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  36. EGFR inhibitor

    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  37. EGFR inhibitor

    DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively.
  38. RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  39. HER2 inhibitor

    TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM.
  40. SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
  41. EGFR/HER2 dual inhibitor

    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  42. Epidermal Growth Factor Receptor Peptide (985-996) exists on the cell surface and is activated by the binding of its specific ligands, including epidermal growth factor and transforming growth factor.
  43. EGFR inhibitor

    Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.
  44. EGFR inhibitor

    Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
  45. EGFR inhibitor

    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
  46. 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.
  47. VEGFR/EGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
  48. HER2 inhibitor

    D-69491 (SU11464) is a small-molecule HER2 inhibitor, which was under development for the treatment of tumours with high expression of HER2, such as breast, ovarian, lung and pancreatic carcinomas.
  49. EGFR inhibitor

    AV-412 (MP412) 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.
  50. EGFR/Cdk2 inhibitor

    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

Items 401-450 of 493

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