S2111 |
Lapatinib
|
Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death. |
-
Drug Resist Updat, 2024, 73:101066
-
J Extracell Vesicles, 2024, 13(7):e12494
-
Cancer Lett, 2024, 593:216968
|
|
S1011 |
Afatinib
|
アファチニブ (Afatinib) は in vitro において EGFR/ErbB を不可逆的に阻害します。IC50 は EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4) に対してそれぞれ 0.5, 0.4, 10, 14 および 1 nM です。アファチニブによってオートファジー (autophagy) が誘発されることが報告されています。 |
-
Cell, 2024, 187(3):712-732.e38
-
Cell, 2024, S0092-8674(24)00825-0
-
Signal Transduct Target Ther, 2024, 9(1):65
|
|
S7810 |
Afatinib Dimaleate
|
Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy. |
-
Cell, 2024, 187(3):712-732.e38
-
Signal Transduct Target Ther, 2024, 9(1):153
-
J Invest Dermatol, 2024, S0022-202X(23)03210-4
|
|
S1028 |
Lapatinib Ditosylate
|
Lapatinib Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. |
-
NPJ Breast Cancer, 2024, 10(1):65
-
iScience, 2024, 27(2):108839
-
STAR Protoc, 2024, 5(2):102987
|
|
S1167 |
CP-724714
|
CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2. |
-
Front Immunol, 2024, 15:1335302
-
Cells, 2024, 13(17)1452
-
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
|
|
S2150 |
Neratinib
|
Neratinib is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. |
-
Oncogenesis, 2024, 13(1):30
-
World J Oncol, 2024, 15(3):492-505
-
World J Oncol, 2024, 15(2):192-208
|
|
S2727 |
Dacomitinib
|
Dacomitinib is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2. |
-
Nat Commun, 2024, 15(1):2742
-
Cell Rep Med, 2024, 5(7):101615
-
Drug Dev Res, 2024, 85(5):e22232
|
|
S2192 |
Sapitinib (AZD8931)
|
Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2. |
-
Front Cell Infect Microbiol, 2024, 14:1367938
-
Cell Death Dis, 2023, 14(8):532
-
Adv Sci (Weinh), 2022, e2201539
|
|
S1019 |
Canertinib (CI-1033)
|
Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. |
-
Cells, 2022, 11(3)425
-
Cells, 2022, 11(3)425
-
Front Mol Biosci, 2022, 9:952651
|
|
S5241 |
Lapatinib ditosylate monohydrate
|
Lapatinib ditosylate monohydrate (Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate, Lapatinib tosilate hydrate) is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways, used for treatment of solid tumours such as breast and lung cancer. |
-
Int J Biol Macromol, 2024, 282(Pt 2):136760
-
Int J Mol Sci, 2023, 24(7)6228
-
Biochem Biophys Rep, 2023, 34:101436
|
|
S2250 |
EGCG ((-)-Epigallocatechin Gallate)
|
EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity. |
-
Journal of Functional Foods, 2024, 105977
-
Cell Rep Med, 2023, 4(5):101026
-
Transl Oncol, 2023, 35:101712
|
|
S2216 |
Mubritinib (TAK 165)
|
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. |
-
Sci Adv, 2024, 10(12):eadl4018
-
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
-
Biochem Biophys Rep, 2023, 34:101436
|
|
S7358 |
Poziotinib
|
Poziotinib is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2. |
-
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
-
iScience, 2024, 27(2):108839
-
Int J Mol Sci, 2024, 25(7)3992
|
|
A2007 |
Trastuzumab (anti-HER2)
|
Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD. |
-
Cell Death Dis, 2024, 15(7):480
-
Eur J Med Chem, 2024, 264:116014
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(8):167458
|
|
S1194 |
CUDC-101
|
CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
-
Nat Commun, 2023, 14(1):2095
-
Nat Commun, 2023, 14(1):2095
-
J Transl Med, 2023, 21(1):604
|
|
S8362 |
Tucatinib
|
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. |
-
Oncogenesis, 2024, 13(1):30
-
Transl Oncol, 2024, 49:102073
-
J Thorac Oncol, 2023, S1556-0864(23)00802-X
|
|
S1486 |
AEE788 (NVP-AEE788)
|
AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. |
-
Cell Rep Med, 2022, 3(1):100492
-
Genome Med, 2020, 18;12(1):17
-
Oncotarget, 2019, 10(68):7185-7197
|
|
S1056 |
AC480 (BMS-599626)
|
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1. |
-
Int J Mol Sci, 2022, 23(22)14023
-
Genome Med, 2020, 18;12(1):17
-
Oncotarget, 2016, 7(24):36956-36970
|
|
A2008 |
Pertuzumab (anti-HER2)
|
Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD. |
-
Cell Death Dis, 2024, 15(7):480
-
Molecules, 2024, 29(21)5117
-
Int J Mol Sci, 2023, 24(7)6791
|
|
S2784 |
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, Aurora B, Lck, CSK etc. Phase 1. |
-
Oncotarget, 2020, 11(46):4224-4242
-
Mol Pharmacol, 2019, 95(5):528-536
-
Sci Signal, 2018, 11(549)
|
|
S2816 |
Tyrphostin AG 879
|
Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR. |
-
Nat Commun, 2023, 14(1):1516
-
Nat Commun, 2023, 14(1):1516
-
Br J Pharmacol, 2015, 172(13):3370-82
|
|
S8852 |
Pyrotinib dimaleate
|
Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively. |
-
Transl Oncol, 2024, 49:102073
-
Transl Lung Cancer Res, 2021, 10(8):3659-3670
-
Biomed Chromatogr, 2021, e5221
|
|
S6813 |
Mobocertinib (TAK788)
|
Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent. |
-
Int J Mol Sci, 2024, 25(7)3992
-
J Thorac Oncol, 2023, S1556-0864(23)00797-9
-
Lung Cancer, 2020, 152:135-142
|
|
S2752 |
HER2-Inhibitor-1
|
HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. |
-
Commun Biol, 2021, 4(1):762
|
|
S0290 |
SU5204
|
SU5204, an analogue of SU5025, is a pharmacological inhibitor of VEGFR2. |
-
Front Pharmacol, 2021, 12:804327
|
|
S8833 |
TAS0728
|
TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity. |
-
J Thorac Oncol, 2023, S1556-0864(23)00802-X
|
|
S9786 |
Tuxobertinib (BDTX-189)
|
Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity. |
-
Chem Biol Interact, 2024, 395:111033
-
J Transl Med, 2023, 21(1):89
-
J Transl Med, 2023, 21(1):89
|
|
S3984 |
Nordihydroguaiaretic acid (NDGA)
|
Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis. |
|
|
E4819New |
Afatinib free base
|
Afatinib free base (Gilotrif, BIBW2992, Boehringer Ingelheim) is a second-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 14 nM and 1 nM for wild-type EGFR, EGFR-L858R, HER2, ErbB4, respectively. |
|
|
S6805 |
Tyrphostin AG-528
|
Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity. |
|
|
A2606 |
Disitamab (Anti-ERBB2 / HER2 / CD340)
|
Disitamab (Anti-ERBB2 / HER2 / CD340) is a humanized monoclonal antibody targeting HER2. It can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin. It has antitumor and antineoplastic activities. MW :144.16 KD |
|
|
E1791New |
Zongertinib
|
Zongertinib (BI 1810631, BI 764532) is a selective and potent inhibitor of human HER2 and EGFR tyrosine kinase that covalently binds to both wild-type and mutated HER2 receptors, including exon 20 insertion mutations, while sparing EGFR signaling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumors. |
|
|
A2899 |
Margetuximab (Anti-ERBB2 / HER2 / CD340)
|
Margetuximab (Anti-ERBB2 / HER2 / CD340) is a Fc-domain optimized IgG monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activities. MW: 146.1 KD. |
|
|
A2660 |
Seribantumab (Anti-ERBB3 / HER3)
|
Seribantumab (Anti-ERBB3 / HER3) is a fully human IgG2 monoclonal antibody that targets HER3. It inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models. MW : 143.14 KD. |
|
|
D4001 |
Trastuzumab deruxtecan (DS-8201a, T-DXd)
|
Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. Trastuzumab deruxtecan has a molecular weight of 153KDa. |
|
|
D4003 |
Trastuzumab Emtansine(T-DM1)
|
Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution. |
|
|
A2506 |
Patritumab (Anti-ERBB3 / HER3)
|
Patritumab (Anti-ERBB3 / HER3) is a neutralizing monoclonal antibody targeting ERBB3. Patritumab shows a synergy with Cetuximab, potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors. MW: 145.5 KD. |
|
|
E0200 |
Trastuzumab-deruxtecan (DS-8201a, T-DXd)
|
Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. This product is supplied as 10mg/ml PBS solution. |
|
|
S6897 |
Epertinib hydrochloride
|
Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity. |
|
|
E2851 |
Trastuzumab-Emtansine(T-DM1)
|
Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.This product is supplied as 10mg/ml PBS solution. |
|
|
D4049 |
Disitamab vedotin
|
Disitamab Vedotin (RC-48 ,RC 480-ADC) is an antibody-drug conjugate(ADC) composed of anti-[ERBB2 (epidermal growth factor receptor 2, receptor tyrosine-protein kinase erbB-2, EGFR2, HER2, HER-2, p185c-erbB2, NEU, CD340)] humanized monoclonal antibody, conjugated to monomethylauristatin E (MMAE), via a cleavable maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker. Disitamab Vedotin has the potential for use in solid tumors mainly in advanced breast cancer. |
|
|
D4052 |
Trastuzumab MMAE
|
Trastuzumab MMAE is an antibody-drug conjugate (ADC). It is composed of monomethyl auristatin E (MMAE) and trastuzumab conjugated via a Vc (Valine‐citrulline) linker. Trastuzumab MMAE has high affinity, specificity and anti-tumor activity in vitro. |
|
|
S2111 |
Lapatinib
|
Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death. |
- Drug Resist Updat, 2024, 73:101066
- J Extracell Vesicles, 2024, 13(7):e12494
- Cancer Lett, 2024, 593:216968
|
|
S1011 |
Afatinib
|
アファチニブ (Afatinib) は in vitro において EGFR/ErbB を不可逆的に阻害します。IC50 は EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4) に対してそれぞれ 0.5, 0.4, 10, 14 および 1 nM です。アファチニブによってオートファジー (autophagy) が誘発されることが報告されています。 |
- Cell, 2024, 187(3):712-732.e38
- Cell, 2024, S0092-8674(24)00825-0
- Signal Transduct Target Ther, 2024, 9(1):65
|
|
S7810 |
Afatinib Dimaleate
|
Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy. |
- Cell, 2024, 187(3):712-732.e38
- Signal Transduct Target Ther, 2024, 9(1):153
- J Invest Dermatol, 2024, S0022-202X(23)03210-4
|
|
S1028 |
Lapatinib Ditosylate
|
Lapatinib Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. |
- NPJ Breast Cancer, 2024, 10(1):65
- iScience, 2024, 27(2):108839
- STAR Protoc, 2024, 5(2):102987
|
|
S1167 |
CP-724714
|
CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2. |
- Front Immunol, 2024, 15:1335302
- Cells, 2024, 13(17)1452
- Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
|
|
S2150 |
Neratinib
|
Neratinib is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. |
- Oncogenesis, 2024, 13(1):30
- World J Oncol, 2024, 15(3):492-505
- World J Oncol, 2024, 15(2):192-208
|
|
S2727 |
Dacomitinib
|
Dacomitinib is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2. |
- Nat Commun, 2024, 15(1):2742
- Cell Rep Med, 2024, 5(7):101615
- Drug Dev Res, 2024, 85(5):e22232
|
|
S2192 |
Sapitinib (AZD8931)
|
Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2. |
- Front Cell Infect Microbiol, 2024, 14:1367938
- Cell Death Dis, 2023, 14(8):532
- Adv Sci (Weinh), 2022, e2201539
|
|
S1019 |
Canertinib (CI-1033)
|
Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. |
- Cells, 2022, 11(3)425
- Cells, 2022, 11(3)425
- Front Mol Biosci, 2022, 9:952651
|
|
S5241 |
Lapatinib ditosylate monohydrate
|
Lapatinib ditosylate monohydrate (Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate, Lapatinib tosilate hydrate) is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways, used for treatment of solid tumours such as breast and lung cancer. |
- Int J Biol Macromol, 2024, 282(Pt 2):136760
- Int J Mol Sci, 2023, 24(7)6228
- Biochem Biophys Rep, 2023, 34:101436
|
|
S2250 |
EGCG ((-)-Epigallocatechin Gallate)
|
EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity. |
- Journal of Functional Foods, 2024, 105977
- Cell Rep Med, 2023, 4(5):101026
- Transl Oncol, 2023, 35:101712
|
|
S2216 |
Mubritinib (TAK 165)
|
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. |
- Sci Adv, 2024, 10(12):eadl4018
- Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
- Biochem Biophys Rep, 2023, 34:101436
|
|
S7358 |
Poziotinib
|
Poziotinib is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2. |
- Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
- iScience, 2024, 27(2):108839
- Int J Mol Sci, 2024, 25(7)3992
|
|
S1194 |
CUDC-101
|
CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
- Nat Commun, 2023, 14(1):2095
- Nat Commun, 2023, 14(1):2095
- J Transl Med, 2023, 21(1):604
|
|
S8362 |
Tucatinib
|
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. |
- Oncogenesis, 2024, 13(1):30
- Transl Oncol, 2024, 49:102073
- J Thorac Oncol, 2023, S1556-0864(23)00802-X
|
|
S1486 |
AEE788 (NVP-AEE788)
|
AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. |
- Cell Rep Med, 2022, 3(1):100492
- Genome Med, 2020, 18;12(1):17
- Oncotarget, 2019, 10(68):7185-7197
|
|
S1056 |
AC480 (BMS-599626)
|
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1. |
- Int J Mol Sci, 2022, 23(22)14023
- Genome Med, 2020, 18;12(1):17
- Oncotarget, 2016, 7(24):36956-36970
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S2784 |
TAK-285
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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. |
- Oncotarget, 2020, 11(46):4224-4242
- Mol Pharmacol, 2019, 95(5):528-536
- Sci Signal, 2018, 11(549)
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S2816 |
Tyrphostin AG 879
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Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR. |
- Nat Commun, 2023, 14(1):1516
- Nat Commun, 2023, 14(1):1516
- Br J Pharmacol, 2015, 172(13):3370-82
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S8852 |
Pyrotinib dimaleate
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Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively. |
- Transl Oncol, 2024, 49:102073
- Transl Lung Cancer Res, 2021, 10(8):3659-3670
- Biomed Chromatogr, 2021, e5221
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S6813 |
Mobocertinib (TAK788)
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Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent. |
- Int J Mol Sci, 2024, 25(7)3992
- J Thorac Oncol, 2023, S1556-0864(23)00797-9
- Lung Cancer, 2020, 152:135-142
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S2752 |
HER2-Inhibitor-1
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HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. |
- Commun Biol, 2021, 4(1):762
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S0290 |
SU5204
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SU5204, an analogue of SU5025, is a pharmacological inhibitor of VEGFR2. |
- Front Pharmacol, 2021, 12:804327
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S8833 |
TAS0728
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TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity. |
- J Thorac Oncol, 2023, S1556-0864(23)00802-X
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S9786 |
Tuxobertinib (BDTX-189)
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Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity. |
- Chem Biol Interact, 2024, 395:111033
- J Transl Med, 2023, 21(1):89
- J Transl Med, 2023, 21(1):89
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S3984 |
Nordihydroguaiaretic acid (NDGA)
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Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis. |
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E4819New |
Afatinib free base
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Afatinib free base (Gilotrif, BIBW2992, Boehringer Ingelheim) is a second-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 14 nM and 1 nM for wild-type EGFR, EGFR-L858R, HER2, ErbB4, respectively. |
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S6805 |
Tyrphostin AG-528
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Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity. |
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E1791New |
Zongertinib
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Zongertinib (BI 1810631, BI 764532) is a selective and potent inhibitor of human HER2 and EGFR tyrosine kinase that covalently binds to both wild-type and mutated HER2 receptors, including exon 20 insertion mutations, while sparing EGFR signaling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumors. |
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D4001 |
Trastuzumab deruxtecan (DS-8201a, T-DXd)
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Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. Trastuzumab deruxtecan has a molecular weight of 153KDa. |
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D4003 |
Trastuzumab Emtansine(T-DM1)
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Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution. |
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E0200 |
Trastuzumab-deruxtecan (DS-8201a, T-DXd)
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Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. This product is supplied as 10mg/ml PBS solution. |
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S6897 |
Epertinib hydrochloride
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Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity. |
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E2851 |
Trastuzumab-Emtansine(T-DM1)
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Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.This product is supplied as 10mg/ml PBS solution. |
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