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 101-125 of 531

  • AG 555
    Cat. No.
    A18337

    AG 555

    Synonyms: Tyrphostin AG 555

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

    5 mg
    $30.00
    10 mg
    $55.00
    All 6 sizes
  • TQB3804
    Cat. No.
    A18562

    TQB3804 (EGFR-IN-7)

    Synonyms: EGFR-IN-7

    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.

    1 mg
    $90.00
    5 mg
    $235.00
    All 7 sizes
  • Mutated EGFR-IN-2
    Cat. No.
    A18565

    Mutated EGFR-IN-2

    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 ≤ 1 nM) 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.

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes
  • DBPR112
    Cat. No.
    A18857

    DBPR112

    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.

    1 mg
    $60.00
    5 mg
    $165.00
    All 7 sizes
  • RTC-5
    Cat. No.
    A19067

    RTC-5

    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.

    5 mg
    $40.00
    10 mg
    $70.00
    All 7 sizes
  • TAS0728
    Cat. No.
    A19382

    TAS0728

    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.

    1 mg
    $35.00
    5 mg
    $105.00
    All 8 sizes
  • SDZ281-977
    Cat. No.
    A19410

    SDZ281-977

    Synonyms: SDZ-LAP 977

    SDZ281-977 is an antiproliferative agent. It acts by binding to the “colchicine binding site” on tubulin and inhibiting tubulin polymerization in vitro.

    1 mg
    $95.00
    5 mg
    $240.00
    All 7 sizes
  • Pyrotinib
    Cat. No.
    A19423

    Pyrotinib

    Synonyms: SHR-1258

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

    1 mg
    $200.00
    5 mg
    $610.00
    All 5 sizes
  • Zipalertinib
    Cat. No.
    A19541

    Zipalertinib (TAS6417)

    Synonyms: TAS 6417

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

    1 mg
    $80.00
    2 mg
    $120.00
    All 9 sizes
  • EGFR-IN-5
    Cat. No.
    A20082

    EGFR-IN-5

    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.

    1 mg
    $100.00
    5 mg
    $255.00
    All 7 sizes
  • RG13022
    Cat. No.
    A20455

    RG13022

    Synonyms: Tyrphostin RG13022

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

    2 mg
    $30.00
    5 mg
    $50.00
    All 7 sizes
  • Mutated EGFR-IN-1
    Cat. No.
    A20555

    Mutated EGFR-IN-1 (Osimertinib analog)

    Synonyms: Osimertinib analog

    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.

    5 mg
    $25.00
    10 mg
    $45.00
    All 8 sizes
  • NRC-2694
    Cat. No.
    A20643

    NRC-2694

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

    1 mg
    $70.00
    5 mg
    $155.00
    All 8 sizes
  • Naquotinib mesylate
    Cat. No.
    A20762

    Naquotinib mesylate

    Synonyms: ASP8273 (mesylate); ASP 8273

    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.

    1 mg
    $30.00
    2 mg
    $50.00
    All 7 sizes
  • rel-Lifirafenib
    Cat. No.
    A20988

    rel-Lifirafenib

    Synonyms: BGB-283

    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.

    5 mg
    $140.00
    10 mg
    $242.00
    All 4 sizes
  • Mutant EGFR inhibitor
    Cat. No.
    A21144

    Mutant 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.

    1 mg
    $25.00
    2 mg
    $35.00
    All 8 sizes
  • BGB-102
    Cat. No.
    A21288

    BGB-102

    Synonyms: JNJ-26483327

    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.

    1 mg
    $320.00
    5 mg
    $810.00
    All 5 sizes
  • Almonertinib hydrochloride
    Cat. No.
    A21661

    Almonertinib hydrochloride (HS-10296)

    Synonyms: HS10296

    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.

    1 mg
    $85.00
    5 mg
    $190.00
    All 7 sizes
  • BMS-599626
    Cat. No.
    A21664

    BMS-599626

    Synonyms: AC480

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

    1 mg
    $90.00
    5 mg
    $290.00
    All 4 sizes
  • Nazartinib mesylate
    Cat. No.
    A21741

    Nazartinib mesylate

    Synonyms: EGF816 (mesylate); EGF 816

    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.

    1 mg
    $200.00
    5 mg
    $500.00
    All 6 sizes
  • Nazartinib S-enantiomer
    Cat. No.
    A21747

    Nazartinib S-enantiomer

    Synonyms: EGF816 (S-enantiomer); EGF 816

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

    1 mg
    $345.00
    2 mg
    $535.00
    All 6 sizes
  • Pyrotinib dimaleate
    Cat. No.
    A21756

    Pyrotinib dimaleate

    Synonyms: SHR-1258 dimaleate; SHR1258

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

    1 mg
    $150.00
    5 mg
    $475.00
    All 7 sizes

Items 101-125 of 531

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