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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.

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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Rilzabrutinib
T125421575596-29-0
Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.
  • $100
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TargetMol | Inhibitor Hot
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
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
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.
  • $84
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Pyrotinib dimaleate
T125941397922-61-0In house
Pyrotinib dimaleate is a selective EGFR HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.
  • $157
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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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CUDC-101
T31081012054-59-9
CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.
  • $43
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Zenocutuzumab
T769481969309-56-5
Zenocutuzumab (MCLA-128) is a humanized antibody targeting the extracellular domains of HER2 and HER3. It can be used for research on tumors driven by NRG1 gene rearrangement.
  • $396
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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.
  • $179
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MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate
T744682413016-49-4In house
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate is a conjugate of MC-Val-Cit-PAB-Amide and TLR7 agonist 4, used in cancer research.
  • $195
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(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.
  • $30
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TargetMol | Citations Cited
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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Afatinib Dimaleate
T1773850140-73-7
Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
  • $34
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TargetMol | Citations Cited
Tarloxotinib bromide
T130881636180-98-7
Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR HER2.
  • $143
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(S)-Sunvozertinib
T93042370013-49-1
(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR HER2 inhibitor.
  • $57
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ARRY-380 (analog )
T2518937265-83-3
ARRY-380 analog (HER2-Inhibitor-1) is a potent and selective HER2 inhibitor.
  • $30
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BMS-690514
T14677859853-30-8
BMS-690514 is a potent, orally active inhibitor of EGFR and VEGFR, with IC50 values of 5 nM for EGFR, 20 nM for HER 2, and 60 nM for HER 4.
  • $142
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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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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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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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Tucatinib hemiethanolate
T366481429755-56-5
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.
  • $40
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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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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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BMS-599626 2HCL(714971-09-2 Free base)
T2610L
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
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varlitinib
T6719845272-21-1
Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.
  • $30
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HyT36
T720751323151-45-6
HyT36 is a small molecule hydrophobic tag that selectively destabilizes and promotes the degradation of fusion proteins and the pseudokinase Her3. HyT36 can treat cells expressing erht induced acutely.
  • $51
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TAK-285
T6039871026-44-7
TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
  • $34
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tas0728
T78192088323-16-2
TAS0728 is a HER2 inhibitor, with antitumor activity
  • $43
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RG14620
T3554136831-49-7
RG14620 (Tyrphostin RG14620) is an epidermal growth factor receptor (EGFR) inhibitor.
  • $30
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BMS 599626 2HCl (873837-23-1(HCl))
T53981781932-33-9
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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Tuxobertinib
T90722414572-47-5
Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.
  • $34
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Tyrphostin AG 879
T6712148741-30-4
Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.
  • $43
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SU5204
T22431186611-11-0
SU5204 (3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one), an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)
  • $29
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BMS-599626 Hydrochloride
T5390873837-23-1
BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors.
  • $37
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Panomifene HCl
T33876L3026790-25-7In house
Panomifene HCl is a selective anti-estrogenic compound with antitumor activity for the treatment of breast cancer.
  • $195
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Inetetamab
T78335
Inetetamab is a humanized monoclonal antibody targeting HER2 receptor domain IV, exhibiting antitumor activity through inducing pyroptosis in lung adenocarcinoma. It is used in studies of HER2-positive metastatic breast cancer.
  • $289
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SYR127063
T34760871026-18-5
SYR127063 (BDBM-92454) (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.
  • $133
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Gancotamab
T770171509928-00-0
Gancotamab (MM-302) is a HER2-targeting polyethylene glycolated liposome that encapsulates adriamycin to facilitate delivery to HER2-overexpressing tumor cells while limiting exposure to non-target tissues, including the heart.Gancotamab has antitumor activity and may be used to study advanced HER2-positive breast cancer.
  • $195
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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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Margetuximab
T766891350624-75-7
Margetuximab (MGAH-22) is a second generation anti-human epidermal growth factor receptor 2 protein (HER2) monoclonal antibody with anti-tumor activity for the study of metastatic HER2-positive breast cancer and for the synthesis of nanomedicines.
  • $183
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Seribantumab
T767911334296-12-6
Seribantumab (MM 121) is a humanized monoclonal antibody targeting HER3, inhibiting NRG1-induced growth in MCF-7 cells and patient-derived breast and lung cancer cells harboring NRG1 fusions or amplifications. It also induces apoptosis in MDA-MB-175-VII and LUAD-0061AS3 cells.
  • $78
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Ebselen oxide
T27235104473-83-8
Ebselen oxide (EB-2), a novel variant of HER2 inhibitor for HER2-positive cancers, is an EB-1 analog with antibacterial and antifungal activity, and has shown cytoprotective effects in vitro in addition to cytoprotective effects against HN2.Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa and inhibits HDAC1, HDAC3, HDAC3, and HDAC3. Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa, inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9, and can be used in the study of fungal infections.
  • TBD
35 days
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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
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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.
  • TBD
35 days
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TargetMol
ABP-102
T9901A-750
ABP-102 (CT P72) is a tetravalent IgG1-[L]-scFv bispecific t-cell adduct (BiTE) that acts as a CD3 modulator and selective HER2 modulator for the selective targeting of HER2 overexpressing tumors. ABP-102 showed cytotoxicity in HER2-overexpressing models of breast and gastric cancers, while significantly decreasing activity against HER2 low level cells, twice as effective as rununmotamab.
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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
1-2 weeks
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