EGFR/HER2

EGFR and HER2 inhibitors act on two closely related receptor tyrosine kinases of the ErbB family. The epidermal growth factor receptor (EGFR, ErbB1) and human epidermal growth factor receptor 2 (HER2, ErbB2) form dimers with each other and with ErbB3 and ErbB4. Receptor activation engages the mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K) pathways that control cell growth. Activating EGFR mutations in non-small-cell lung cancer have made the receptor a central model in kinase inhibitor research. Gefitinib and erlotinib are reversible EGFR inhibitors, and lapatinib inhibits both EGFR and HER2. Osimertinib binds covalently to EGFR carrying the T790M resistance mutation, and neratinib irreversibly inhibits HER2 and EGFR.

Items 526-531 of 531

  • EGFR/ACK1-IN-1
    Cat. No.
    A84661

    EGFR/ACK1-IN-1

    EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors.

    5 mg
    $115.00
    10 mg
    $195.00
    All 4 sizes
  • JI-101 hydrochloride
    Cat. No.
    A84699

    JI-101 hydrochloride

    JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms.

    Out of stock

    All 3 sizes
  • (+)-Theta-cypermethrin
    Cat. No.
    B10869

    (+)-Theta-cypermethrin

    (+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology.

    Out of stock

    All 3 sizes
  • Cyclo[K(N3)larllt]
    Cat. No.
    B21825

    Cyclo[K(N3)larllt]

    Cyclo[K(N3)larllt] is a cyclic peptide that specifically targets the epidermal growth factor receptor (EGFR) with a Kd value of 5.09 μM and demonstrates selectivity for related proteins HER2 and HER3. This compound exhibits no cytotoxicity and does not inhibit the growth of EGFR-overexpressing cancer cells. Cyclo[K(N3)larllt] is ideal for use as a ligand in EGFR-targeted fluorescent conjugates, facilitating the detection of tumors with elevated EGFR levels. Its applications extend to research focused on colorectal cancer and related pathologies.

    Out of stock

    All 3 sizes
  • ZW-49
    Cat. No.
    B21999

    ZW-49

    ZW-49 is a potent orally active pan-EGFR inhibitor, demonstrating IC50 values ranging from 0.03 to 1.5 nM. This compound selectively targets various EGFR mutations while sparing wild-type EGFR and other familial targets, effectively blocking the ATP-binding pocket and a conserved hydrophobic subpocket without causing steric conflicts with PACC mutation P loops. ZW-49 exhibits significant anti-proliferative activity by inhibiting cancer cell proliferation, inducing G0/G1 phase cell-cycle arrest, and promoting apoptosis, making it a valuable reagent for cancer research, particularly in non-small cell lung cancer models.

    Out of stock

    All 3 sizes
  • Rinumafusp alfa
    Cat. No.
    B22000

    Rinumafusp alfa

    Rinumafusp alfa is a human monoclonal antibody that specifically inhibits the epidermal growth factor receptor (EGFR) by targeting ERBB3/HER3. This compound demonstrates potential in blocking tumor cell signaling pathways, thereby impeding tumor growth and progression. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting EGFR-related pathways.

    Out of stock

    All 3 sizes

Items 526-531 of 531

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