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Angiogenesis HER

HER

HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. Amplification or over-expression of this oncogene has been shown to play an important role in the development and progression of certain aggressive types of breast cancer. In recent years the protein has become an important biomarker and target of therapy for approximately 30% of breast cancer patients.
Cat No. product name
T2325 NeratinibHOT Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
T2303 AfatinibHOT 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...
T9072 BDTX-189 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...
T6039 TAK285 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...
T2630 Poziotinib Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
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.
T3554 RG 14620 RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
T0801 Tannic acid Tannic acid is a novel hERG channel blocker.
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.
T2047 AG1478 AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
T3192 NS1643 NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
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...
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 ...
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...
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...
T22431 SU5204 SU5204, an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)
T2364 Irbinitinib Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
T2518 ARRY380 ARRY-380 is a potent and selective HER2 inhibitor.
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.
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 i...
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...
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...
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.
T7819 TAS0728 TAS0728 is a HER2 inhibitor, with antitumor activity
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.
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).
T3108 CUDC101 CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
Neratinib HOT
T2325CAS 698387-09-6
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
Afatinib HOT
T2303CAS 439081-18-2
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...
BDTX-189
T9072CAS 2414572-47-5
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...
TAK285
T6039CAS 871026-44-7
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, Auro...
Poziotinib
T2630CAS 1092364-38-9
Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
Endoxifen Z-isomer
T2280CAS 112093-28-4
Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
RG 14620
T3554CAS 136831-49-7
RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
Tannic acid
T0801CAS 1401-55-4
Tannic acid is a novel hERG channel blocker.
Tyrphostin AG 879
T6712CAS 148741-30-4
Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
AG1478
T2047CAS 153436-53-4
AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
NS1643
T3192CAS 448895-37-2
NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
Terfenadine
T1266CAS 50679-08-8
Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistamin...
Mollugin
T3673CAS 55481-88-4
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 ...
BMS 599626
T2610CAS 714971-09-2
BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
Afatinib Dimaleate
T1773CAS 850140-73-7
Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGF...
PF04929113
T6341CAS 908115-27-5
SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned...
SU5204
T22431CAS 186611-11-0
SU5204, an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)
Irbinitinib
T2364CAS 937263-43-9
Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
ARRY380
T2518CAS 937265-83-3
ARRY-380 is a potent and selective HER2 inhibitor.
PF-04929113 Mesylate
T4342CAS 1173111-67-5
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
T4075CAS 1816307-67-1
Sulfatinib may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity. It also is a hERG inhibitor.
Furanodienone
T4S0544CAS 24268-41-5
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 i...
NS309
T4612CAS 18711-16-5
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...
NS309
T4612CAS 18711-16-5
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...
BMS 599626 2HCl (873837-23-1(HCl))
T5398CAS 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.
TAS0728
T7819CAS 2088323-16-2
TAS0728 is a HER2 inhibitor, with antitumor activity
BMS-690514
T14677CAS 859853-30-8
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.
Epertinib
T11213LCAS 908305-13-5
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 ...
Epertinib hydrochloride
T11213CAS 2071195-74-7
Epertinib hydrochloride shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor...
BGB-102
T10531CAS 807640-87-5
BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM).
CUDC101
T3108CAS 1012054-59-9
CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.