EGFR/HER2

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  1. EGFR T790M inhibitor

    EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.
  2. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  3. 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.
  4. EGFR inhbitor

    EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
  5. EGFR inhibitor

    Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.
  6. EGFR inhibitor

    PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
  7. ALK/EGFR inhibitor

    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
  8. Her3 (ErbB3) ligand

    TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function.
  9. HER2 inhibitor

    ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
  10. EGFR activator

    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR.
  11. irreversible EGFR inhibitor

    Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
  12. 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.
  13. 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.
  14. T790M-Containing EGFR Mutants inhibitor

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

    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
  16. 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.
  17. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. tyrosine kinase inhibitor

    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
  30. EGFR/HER2 dual inhibitor

    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  31. 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.
  32. EGFR inhibitor

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

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

    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
  35. 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.
  36. VEGFR/EGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
  37. 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.
  38. 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.
  39. EGFR/Cdk2 inhibitor

    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
  40. 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.
  41. 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.
  42. EGFR/HER2 dual inhibitor

    Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
  43. EGFR inhibitor

    Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor.
  44. EGFR inhibitor

    Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).
  45. EGFR inhibitor

    AG-99 is an epidermal growth factor receptor (EGFR) kinase inhibitor with IC50 value of 10 μM.
  46. EGFR inhibitor

    AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells.
  47. EGFR inhibitor

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
  48. EGFR/PI3K dual inhibitor

    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.
  49. EGFR inhibitor

    RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
  50. EGFR inhibitor

    AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor.

Items 51-100 of 493

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