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HER

The human epidermal growth factor receptor (HER) family of receptors plays a central role in the pathogenesis of several human cancers. They regulate cell growth, survival, and differentiation via multiple signal transduction pathways and participate in cellular proliferation and differentiation.

  • Neratinib
    T2325698387-09-6
    Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
    • $30
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    TargetMol | Citations Cited
  • PF-04929113 Mesylate
    T43421173111-67-5
    PF-04929113 Mesylate (SNX-5422 Mesylate), a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).
    • $71
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  • BMS 599626 2HCl (873837-23-1(HCl))
    T5398
    BMS 599626 2HCl (873837-23-1(HCl)) (AC480 dihydrochloride) is a selective inhibitor of HER1 and HER2 (IC50s: 20 nM and 30 nM), ~8-fold less potent to HER4, >100-fold to Lck, VEGFR2, c-Kit, MET, etc.
    • $50
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  • BMS-599626 2HCL(714971-09-2 Free base)
    T2610L1781932-33-9
    BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.
    • $86
    In Stock
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  • Terodiline
    T6053615793-40-5In house
    Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.
    • $293
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    TargetMol | Inhibitor Sale
  • Panomifene HCl
    T33876L In house
    Panomifene HCl is a selective anti-estrogenic compound with antitumor activity for the treatment of breast cancer.
    • $195
    In Stock
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    TargetMol | Inhibitor Sale
  • SYR127063
    T34760871026-18-5
    SYR127063 (BDBM-92454) (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.
    • $133
    In Stock
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    TargetMol | Inhibitor Sale
  • Sarizotan 2HCl
    T70044L177976-12-4In house
    Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.
    • $195
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    TargetMol | Inhibitor Sale
  • Sulcardine 2HCl
    T83979343935-48-8In house
    Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.
    • $195
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  • AG-1557 hydrochloride (189290-58-2(free base))
    T4694
    AG-1557 hydrochloride is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
    • $33
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    TargetMol | Inhibitor Sale
  • Sarizotan HCl
    T70044195068-07-6In house
    Sarizotan HCl (EMD 128130 HCl) is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinson's Dyskinesia.
    • $293
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    TargetMol | Inhibitor Sale
  • EGFR-IN-99
    T359012068806-31-3
    EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).
    • $129
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    TargetMol | Inhibitor Sale
  • NP10679
    T734472914889-88-4In house
    NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.
    • $293 TargetMol
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    TargetMol | Inhibitor Sale
  • Zongertinib
    T695342728667-27-2In house
    Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.
    • $148
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  • Sigma-1 receptor antagonist 3
    T129121639220-17-9In house
    Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.
    • $98
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    TargetMol | Inhibitor Sale
  • PD-118057
    T16444313674-97-4In house
    PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.
    • $97
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    TargetMol | Inhibitor Sale
  • (S)-Afatinib
    T2303439081-18-2
    (S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.
    • $29
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    TargetMol | Citations Cited
  • AG-1478
    T2047153436-53-4
    AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
    • $45
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    TargetMol | Citations Cited
  • Tucatinib
    T2364937263-43-9
    Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
    • $30
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    TargetMol | Citations Cited
  • AZD7507
    T143801041852-85-0
    AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.
    • $84
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    TargetMol | Inhibitor Sale
  • ARRY-380 (analog )
    T2518937265-83-3
    ARRY-380 analog (HER2-Inhibitor-1) is a potent and selective HER2 inhibitor.
    • $30
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    TargetMol | Inhibitor Sale
  • Patritumab
    T767961262787-83-6
    Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-small cell lung cancer.
    • $297
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    TargetMol | Inhibitor Sale
  • RG14620
    T3554136831-49-7
    RG14620 (Tyrphostin RG14620) is an epidermal growth factor receptor (EGFR) inhibitor.
    • $30
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    TargetMol | Inhibitor Sale
  • NS309
    T461218711-16-5
    NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE
    • $52
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    TargetMol | Inhibitor Sale
  • Guanfu base A
    T81821394-48-5
    Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.
    • $97
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    TargetMol | Inhibitor Sale
  • HER2/neu (654-662) GP2 acetate
    TP1583L
    HER2/neu (654-662) GP2 acetate is derived from the human epidermal growth factor receptor 2 (HER2-Neu, 654–662). HER2/neu (654-662) GP2 acetate induces HLA-A2-restricted cytotoxic T lymphocytes reactive to various epithelial cancers.
    • $195
    Backorder
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    TargetMol | Inhibitor Sale
  • Epertinib hydrochloride
    T112132071195-74-7
    Epertinib hydrochloride (S-22611 hydrochloride) shows potent antitumor activity. 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.
    • $98
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    TargetMol | Inhibitor Sale
  • Pyrotinib dimaleate
    T125941397922-61-0
    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively.
    • $157
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  • Tannic acid
    T08011401-55-4
    Tannic acid (Gallotannic acid) is a novel hERG channel blocker.
    • $41
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    TargetMol | Citations Cited
  • O-Nornuciferine
    TN10923153-55-7
    O-Nornuciferine reveals distinct in vitro hERG blockages measured in HEK293 cells with the IC50 value of 2.89 uM.
    • $152
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  • Neratinib maleate
    T67385915942-22-2
    Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer.
    • $40
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  • BI-4142
    T636432682003-36-5
    BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.
    • $226
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  • Mollugin
    T367355481-88-4
    Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.
    • $39
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  • BMS-599626
    T2610714971-09-2
    BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
    • $558
    35 days
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  • Dihydroberberine
    T8189483-15-8
    Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces Hsp90 expression and its interaction with hERG.
    • $41
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  • Poziotinib
    T26301092364-38-9
    Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
    • $30
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  • Furanodienone
    T4S054424268-41-5
    1. Furanodienone has effects on MCF-7 cells are mediated, at least in part, by inhibiting ERα signaling. 2. Furanodienone inhibits EGFR/HER2 signaling pathway in BT474 and SKBR3 cells, the effect is specifically dependent on the expression of HER2 but not EGFR .
    • $54
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  • Tucatinib hemiethanolate
    T366481429755-56-5
    Tucatinib hemiethanolate (Irbinitinib hemiethanolate) is an orally active, selective and potent tyrosine kinase inhibitor targeting human epidermal growth factor receptor 2 (HER2) with anticancer activity for the study of metastatic HER2-positive breast and colorectal cancers.
    • $30
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  • Rilzabrutinib
    T125421575596-29-0
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).
    • $118
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  • Tuxobertinib
    T90722414572-47-5
    Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activity.
    • $34
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  • TAS0728
    T78192088323-16-2
    TAS0728 is a HER2 inhibitor, with antitumor activity
    • $72
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  • AG1557
    T2034189290-58-2
    AG1557 (AG-1557) is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
    • $43
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  • PF04929113
    T6341908115-27-5
    PF04929113 (SNX-5422) is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, PF04929113 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.
    • $33
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  • Epertinib
    T11213L908305-13-5
    Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.
    • $1,360
    Backorder
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  • Cisapride
    T129181098-60-4
    Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.
    • $39
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  • Varlitinib
    T6719845272-21-1
    Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
    • $67
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  • NS1643
    T3192448895-37-2
    NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
    • $35
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  • AZD-5672
    T30260780750-65-4
    AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM. AZD-5672 inhibits hERG cardiac ion channel binding and P-gp-mediated digoxin transport with IC50s of 7.3 μM and 32 μM. AZD-5672 can be used in studies about rheumatoid arthritis.
    • $213
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  • BMS-690514
    T14677859853-30-8
    BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
    • $142
    5 days
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  • MCHR1 antagonist 2
    T11966863115-70-2
    MCHR1 antagonist 2 is an antagonist of melanin-concentratin hormone receptor 1(MCH1-R, IC50 = 65 nM) and also inhibits hERG.
    • $147
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