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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.
Cat No. product name
TN1092 O-Nornuciferine O-Nornuciferine reveals distinct in vitro hERG blockages measured in HEK293 cells with the IC50 value of 2.89 uM.
T12912 Sigma-1 receptor antagonist 3 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.
T2047 AG-1478 AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
T9009 ICA-105574 ICA-105574 is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. ...
T8189 Dihydroberberine Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channel...
T14677 BMS-690514 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.
T4694 AG-1557 hydrochloride (189290-58-2(free base)) AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
T9304 (S)-Sunvozertinib DZD9008 is a rationally designed selective, irreversible EGFR/HER2 inhibitor.
T6827 Endoxifen Z-isomer hydrochloride Endoxifen HCl is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.
T2630 Poziotinib Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
T22431 SU5204 SU5204, an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)
T0801 Tannic acid Tannic acid is a novel hERG channel blocker.
T6677 Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
T34760 SYR127063 SYR127063 (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.
T7819 TAS0728 TAS0728 is a HER2 inhibitor, with antitumor activity
T6712 Tyrphostin AG 879 Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
T1266 Terfenadine Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistamin...
T3192 NS1643 NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
T2034 AG1557 AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
T8182 Guanfu base A 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.
T4S0544 Furanodienone 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...
T1291 Cisapride Cisapride is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal pe...
T2280 Endoxifen (Z-isomer) Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
T12542 Rilzabrutinib PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).
T9072 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, reape...
T2610 BMS-599626 BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
T1773 Afatinib Dimaleate Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGF...
T14380 AZD7507 AZD7507 is a CSF-1R inhibitor. It has antitumor activity.
T12594 Pyrotinib dimaleate Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 (IC50 s of 13 and 38 nM, respectively).
T2325 Neratinib Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
T2303 Afatinib Afatinib (BIBW 2992) 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, resp...
T2364 Tucatinib Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
T2518 ARRY-380 (analog ) ARRY-380 is a potent and selective HER2 inhibitor.
T11213L Epertinib 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 ...
T11213 Epertinib hydrochloride Epertinib hydrochloride shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor ...
T10531 BGB-102 BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM).
T3673 Mollugin Mollugin 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 ...
T3554 RG14620 RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
T3108 CUDC-101 CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
T4612 NS309 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 ...
T4342 PF-04929113 Mesylate PF-04929113 Mesylate, a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).
T4075 Sulfatinib Sulfatinib may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity. It also is a hERG inhibitor.
T5398 BMS 599626 2HCl (873837-23-1(HCl)) BMS-599626 (AC480) 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.
T6039 TAK-285 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, Auro...
T6341 PF04929113 SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned...
O-Nornuciferine
TN1092
O-Nornuciferine reveals distinct in vitro hERG blockages measured in HEK293 cells with the IC50 value of 2.89 uM.
Sigma-1 receptor antagonist 3
T12912
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.
AG-1478
T2047
AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
ICA-105574
T9009
ICA-105574 is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. ...
Dihydroberberine
T8189
Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channel...
BMS-690514
T14677
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.
AG-1557 hydrochloride (189290-58-2(free base))
T4694
AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
(S)-Sunvozertinib
T9304
DZD9008 is a rationally designed selective, irreversible EGFR/HER2 inhibitor.
Endoxifen Z-isomer hydrochloride
T6827
Endoxifen HCl is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.
Poziotinib
T2630
Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
SU5204
T22431
SU5204, an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)
Tannic acid
T0801
Tannic acid is a novel hERG channel blocker.
Sophocarpine
T6677
Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
SYR127063
T34760
SYR127063 (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.
TAS0728
T7819
TAS0728 is a HER2 inhibitor, with antitumor activity
Tyrphostin AG 879
T6712
Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
Terfenadine
T1266
Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistamin...
NS1643
T3192
NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
AG1557
T2034
AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
Guanfu base A
T8182
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.
Furanodienone
T4S0544
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 i...
Cisapride
T1291
Cisapride is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal pe...
Endoxifen (Z-isomer)
T2280
Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
Rilzabrutinib
T12542
PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).
Tuxobertinib
T9072
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, reape...
BMS-599626
T2610
BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
Afatinib Dimaleate
T1773
Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGF...
AZD7507
T14380
AZD7507 is a CSF-1R inhibitor. It has antitumor activity.
Pyrotinib dimaleate
T12594
Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 (IC50 s of 13 and 38 nM, respectively).
Neratinib
T2325
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
Afatinib
T2303
Afatinib (BIBW 2992) 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, resp...
Tucatinib
T2364
Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
ARRY-380 (analog )
T2518
ARRY-380 is a potent and selective HER2 inhibitor.
Epertinib
T11213L
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 ...
Epertinib hydrochloride
T11213
Epertinib hydrochloride shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor ...
BGB-102
T10531
BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM).
Mollugin
T3673
Mollugin 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 ...
RG14620
T3554
RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
CUDC-101
T3108
CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
NS309
T4612
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...
PF-04929113 Mesylate
T4342
PF-04929113 Mesylate, a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).
Sulfatinib
T4075
Sulfatinib may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity. It also is a hERG inhibitor.
BMS 599626 2HCl (873837-23-1(HCl))
T5398
BMS-599626 (AC480) 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.
TAK-285
T6039
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, Auro...
PF04929113
T6341
SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned...