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  1. General Info
  2. Effects Info
  3. Reference
Drug Details
01. General Information
Name Tamoxifen
PubChem CID 2733526
Molecular Weight 371.5g/mol
Synonyms

tamoxifen, 10540-29-1, trans-Tamoxifen, Crisafeno, Diemon, Tamoxifene, Citofen, Istubol, Oncomox, Retaxim, Tamoxen, Valodex, Tamoxifeno, Tamoxifenum, Novaldex, Tamoxifen (Z), Mammaton, Tamoxifene [INN-French], Tamoxifenum [INN-Latin], Tamoxifeno [INN-Spanish], Tamoplex, CCRIS 3275, (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine, HSDB 6782, 1-p-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene, 1-para-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene, EINECS 234-118-0, Tamoxifen (INN), NSC-727681, Tamoxifen (Standard), DTXSID1034187, UNII-094ZI81Y45, CHEBI:41774, 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine, CHEMBL83, ICI-47699, Tamizam, 094ZI81Y45, (2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}ethyl)dimethylamine, trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine, (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine (IUPAC), 2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine, C26H29NO, DTXCID9014187, EC 234-118-0, Ethanamine, 2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, (Z)-, Ethanamine, 2-[4-[(1Z)-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethyl-, (Z)-2-[4-(1,2)-DIPHENYL-1-BUTENYL)-PHENOXY]-N,N-DIMETHYLETHANAMINE, (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene, TAMOXIFEN [INN], TAMOXIFEN (IARC), TAMOXIFEN [IARC], (Z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-N,N-dimethylethanamine, (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine, (z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-n,n-dimethylethanamine, Tamoxifene (INN-French), Tamoxifenum (INN-Latin), Tamoxifen [INN:BAN], Tamoxifeno (INN-Spanish), Ethylamine, N,N-dimethyl-2-(p-(1,2-diphenyl-1-butenyl)phenoxy)-, (Z)-, (E/Z)-Tamoxifen, 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethyl-ethanamine, Tamoxifen (1.0 mg/mL in Methanol), Ethanamine, 2-(4-((1Z)-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, [3H]tamoxifen, ETHANAMINE, 2-(4-((1Z)-1,2-DIPHENYL-1-BUTEN-1-YL)PHENOXY)-N,N-DIMETHYL-, Tamoxifen (TN), [3H]-tamoxifen, Tamoplex (TN), SMR000059172, CAS-10540-29-1, TRANS FORM OF TAMOXIFEN, ICI 47699, ,citrate, Z-Tamoxifen, 2-(4-((1Z)-1,2-diphenylbut-1-en-1-yl)phenoxy)-N,N-dimethylethanamine, Ethanamine, 2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-, Tamoxifen, 7, Tocris-0999, 1ya4, Tamoxifen, >=99%, TAMOXIFEN [MI], TAMOXIFEN [HSDB], Prestwick2_000146, Prestwick3_000146, Spectrum5_001417, Spectrum5_002043, TAMOXIFEN [VANDF], UPCMLD-DP027, SCHEMBL4084, TAMOXIFEN [WHO-DD], BIDD:PXR0003, Lopac0_001203, BSPBio_000252, BSPBio_001150, BSPBio_001982, MLS001332535, MLS001332536, BIDD:ER0008, BIDD:GT0009, Tamoxifen, analytical standard, BPBio1_000278, GTPL1016, GTPL5384, BDBM20607, cid_2733526, L02BA01, cMAP_000044, HMS1362J11, HMS1792J11, HMS1990J11, HMS2090N08, HMS2232C12, HMS3261D09, HMS3403J11, HMS3411P04, HY-13757AR, ICI47699, Tox21_201243, Tox21_300539, Tox21_500494, (Z)-2-[p-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine, 1-p-.beta.-Dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene, HB0601, HY-13757A, MFCD00010454, NSC727681, AKOS022143035, AM84324, CCG-205277, DB00675, FD12063, KS-1472, LP00494, SDCCGSBI-0051170.P007, ICI47699;Z-Tamoxifen;trans-Tamoxifen, IDI1_000258, IDI1_002170, QTL1_000079, NCGC00024928-01, NCGC00024928-03, NCGC00024928-04, NCGC00024928-05, NCGC00024928-07, NCGC00024928-08, NCGC00024928-09, NCGC00024928-10, NCGC00024928-11, NCGC00024928-12, NCGC00024928-13, NCGC00024928-14, NCGC00024928-15, NCGC00024928-16, NCGC00024928-17, NCGC00024928-18, NCGC00024928-19, NCGC00024928-39, NCGC00024928-40, NCGC00254455-01, NCGC00258795-01, NCGC00261179-01, AC-35768, BT164438, SBI-0051170.P004, CS-0694848, NS00010353, C07108, D08559, AB00053547-16, AB00053547-17, AB00053547-18, AB00053547_19, AB00053547_20, EN300-1273241, A801229, L024126, Q412178, W-108788, BRD-K93754473-001-02-9, BRD-K93754473-048-04-6, BRD-K93754473-048-05-3, BRD-K93754473-048-10-3, Tamoxifen, certified reference material, TraceCERT(R), Z2527624834, 1-p-beta-dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene, (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)phenoxy)-N,N-dimethylethanamine, (Z)-2-(4-(1,2-diphenylbut-1-en-1-yl)phenoxy)-N,N-dimethylethan-1-amine, (Z)-2-(4-(1,2-diphenylbut-1-en-1-yl)phenoxy)-N,N-dimethylethanamine, 2-[4-[(Z)-1,2-di(phenyl)but-1-enyl]phenoxy]-N,N-dimethylethanamine

Drug Type Small molecule
Formula C₂₆H₂₉NO
SMILES CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
InChI 1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-
InChIKey NKANXQFJJICGDU-QPLCGJKRSA-N
CAS Number 10540-29-1
ChEMBL ID CHEMBL83
ChEBI ID CHEBI:41774
TTD ID D07KSG
Drug Bank ID DB00675
KEGG ID C07108
Toxicity Organism Test Type Route(Dose)
rat LD50 intraperitoneal(165 mg/kg)
mouse LD50 intraperitoneal(254 mg/kg)
rat LD50 oral(322 mg/kg)
Structure 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 282
Pair Name Xanthorrhizol, Tamoxifen
Partner Name Xanthorrhizol
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Gene Regulation Up-regulation Expression MAPK14 hsa1432
Up-regulation Expression PSMD9 hsa5715
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
In Vivo Model Using the MCF-7 implanted nude mice model, it was possible to detect significantly increased tumor volumes, a larger tumor size, and increased protein expression of P38 and P27(Kip1) in the xanthorrhizol + tamoxifen group compared to the tamoxifen-alone group.
Result It can be concluded that while there is no significant herb-drug interaction between xanthorrhizol and tamoxifen in vitro, there is such an interaction in tumor-bearing mice, which provides important information that affects breast cancer treatment translational research.
Combination Pair ID: 806
Pair Name Pterostilbene, Tamoxifen
Partner Name Pterostilbene
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Apoptosis
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
ZR-75-1 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0588
Result Pterostilbene shows an additive inhibitory effect on breast cancer cells when combined with tamoxifen, most likely from augmented cancer cell apoptosis.
Combination Pair ID: 954
Pair Name Pancratistatin, Tamoxifen
Partner Name Pancratistatin
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Mitochondria-mediated apoptosis
Gene Regulation Up-regulation Expression ROS1 hsa6098
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
Result In combination with the anti-estrogen Tamoxifen, PST had a synergic effect
Combination Pair ID: 607
Pair Name Pancratistatin, Tamoxifen
Partner Name Pancratistatin
Disease Info [ICD-11: 2C30] Melanoma Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Up-regulation Expression ROS1 hsa6098
Result Our results indicate that TAM alone does not induce apoptosis in this cell line, but sensitizes the mitochondria, thereby enhancing the effect of PST exposure. In conclusion, combination of two nongenotoxic compounds offers a novel treatment regime for this notoriously resilient form of skin cancer.
Combination Pair ID: 20
Pair Name Narciclasine, Tamoxifen
Partner Name Narciclasine
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Target-->STAT3
Gene Regulation Down-regulation Expression BIRC5 hsa332
Down-regulation Expression CCND1 hsa595
Down-regulation Expression MYC hsa4609
Down-regulation Phosphorylation STAT3 hsa6774
Up-regulation Expression TP53 hsa7157
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
Result Our findings successfully highlight the STAT3 as the direct therapeutic target of Nar in ER-positive breast cancer cells, especially, Nar leaded STAT3 degradation as a promising strategy for the tamoxifen-resistant breast cancer treatment.
Combination Pair ID: 896
Pair Name Methylselenocysteine, Tamoxifen
Partner Name Methylselenocysteine
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Expression CCND1 hsa595
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
In Vivo Model About 5×10⁶ cells suspension in 50 uL sterile PBS were mixed with 100 uL Matrigel and administered within both sides of the inguinal mammary fat pad of NU/NU immune-compromised female ovariectomized mice
Result These findings demonstrate synergistic growth inhibition of ERalpha positive breast cancer xenografts by combination of tamoxifen with organic selenium compounds. Organic selenium may provide added benefit when combined with tamoxifen in adjuvant therapy or prevention.
Combination Pair ID: 430
Pair Name Glabridin, Tamoxifen
Partner Name Glabridin
Disease Info [ICD-11: 2C76] Endometrial cancer Investigative
Gene Regulation Down-regulation Expression BCL2 hsa596
Up-regulation Expression ESR1 hsa2099
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
Ishikawa Endometrial adenocarcinoma Homo sapiens (Human) CVCL_2529
Result These results suggested that the combination of tamoxifen and glabridin has potential to be used as an estrogen replacement drug with a reduced risk of endometrial cancer that has arisen from the intake of tamoxifen.
Combination Pair ID: 1019
Pair Name Ginsenoside Rg3, Tamoxifen
Partner Name Ginsenoside Rg3
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Inhibition-->Glycolysis
Gene Regulation Up-regulation Cleavage CASP3 hsa836
Up-regulation Cleavage PARP1 hsa142
Down-regulation Expression PFKFB3 hsa5209
Down-regulation Expression PFKM hsa5213
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
T-47D Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0553
HEK293T Healthy Homo sapiens (Human) CVCL_0063
In Vivo Model A total of 6×10⁶ cells were suspended in 100 μL of a 1:1 mixture of Matrigel and phosphate-buffered saline (PBS),and then injected into the flanks of nude mice.
Result This study highlights the contribution of Rg3 in enhancing the therapeutic efficacy of TAM in breast cancer, and suggests that targeting TAM-resistant PFKFB3 overexpression may represent a promising strategy to improve the response to combination therapy in breast cancer.
Combination Pair ID: 604
Pair Name Evening primrose oil, Tamoxifen
Partner Name Evening primrose oil
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Inhibition-->Tumor angiogenesis
Gene Regulation Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression CCND1 hsa595
Down-regulation Expression VEGFA hsa7422
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
MDA-MB-231 Breast adenocarcinoma Homo sapiens (Human) CVCL_0062
Result The most significant finding of this study was the confirmation of the anticancer activity of the natural product EPO, which potentiated the activity of the anticancer drug TAM against MCF-7 and MDA-MB-231 BC cell lines through the induction of apoptosis, inhibiting angiogenesis and halting cell proliferation.
Combination Pair ID: 1000
Pair Name Celastrol, Tamoxifen
Partner Name Celastrol
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Mitochondria-mediated apoptosis
Gene Regulation Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Up-regulation Cleavage CASP3 hsa836
Up-regulation Expression CYCS hsa54205
In Vitro Model MDA-MB-231 Breast adenocarcinoma Homo sapiens (Human) CVCL_0062
In Vivo Model The cell concentration was adjusted to 4×10⁷ pieces/mL. The single cell suspension was injected under the fourth pair of breast pads on the right side of nude mice, 0.1 mL for each.
Result CEL can promote apoptosis and enhance the TAM sensitivity in TNBC treatment through a mitochondria-mediated pathway.
Combination Pair ID: 160
Pair Name Celastrol, Tamoxifen
Partner Name Celastrol
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Blockade of cell cycle in G0/G1 phase
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Expression MAP1LC3B hsa81631
Down-regulation Phosphorylation MTOR hsa2475
Up-regulation Expression SQSTM1 hsa8878
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
Result The Synergistic Effects of Celastrol in combination with Tamoxifen on Apoptosis and Autophagy in MCF-7 Cells
Combination Pair ID: 694
Pair Name Carnosic acid, Tamoxifen
Partner Name Carnosic acid
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Up-regulation Expression BAD hsa572
Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression BCL-xL hsa598
Up-regulation Cleavage CASP3 hsa836
Up-regulation Cleavage CASP8 hsa841
Up-regulation Cleavage PARP1 hsa142
Up-regulation Expression TNFRSF10C hsa8794
Up-regulation Expression TNFRSF10D hsa8793
Up-regulation Expression TNFSF10 hsa8743
Up-regulation Expression TP53 hsa7157
Up-regulation Expression TP73 hsa7161
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
T-47D Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0553
In Vivo Model 5×10⁵ MCF-7 cells were subcutaneously injected into the dorsal flanks of athymic nude mice.
Result Our study supplies a novel therapeutic strategy to induce apoptosis for suppressing breast cancer, which was relied on Caspase-3/TRAIL activation.
Combination Pair ID: 863
Pair Name Alpha-Mangostin, Tamoxifen
Partner Name Alpha-Mangostin
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Expression BIRC5 hsa332
Down-regulation Expression CCND1 hsa595
Down-regulation Expression KCNH1 hsa3756
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
T-47D Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0553
Royan N30 Healthy Mus musculus (Mouse) CVCL_9414
Result This study establishes the benefits of incorporating AM as a co-adjuvant for first-line ER+ breast cancer therapy.
Reversing Drug Resistance
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Combination Pair ID: 852
Pair Name Luteolin, Tamoxifen
Partner Name Luteolin
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Gene Regulation Down-regulation Expression CCNE2 hsa9134
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
BT-483 Invasive breast carcinoma Homo sapiens (Human) CVCL_2319
BT-474 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0179
MDA-MB-231 Breast adenocarcinoma Homo sapiens (Human) CVCL_0062
AU565 Breast adenocarcinoma Homo sapiens (Human) CVCL_1074
MCF-10A Healthy Homo sapiens (Human) CVCL_0598
Result The results of this study suggest that luteolin can be used as a chemosensitiser to target the expression level of CCNE2 and that it could be a novel strategy to overcome TAM resistance in breast cancer patients.
03. Reference
No. Title Href
1 In vitro and in vivo effects of xanthorrhizol on human breast cancer MCF-7 cells treated with tamoxifen. J Pharmacol Sci. 2014;125(4):375-85. doi: 10.1254/jphs.14024fp. Click
2 Pterostilbene and tamoxifen show an additive effect against breast cancer in vitro. Am J Surg. 2010 Nov;200(5):577-80. doi: 10.1016/j.amjsurg.2010.07.022. Click
3 Synergy of Pancratistatin and Tamoxifen on breast cancer cells in inducing apoptosis by targeting mitochondria. Cancer Biol Ther. 2008 Mar;7(3):376-84. doi: 10.4161/cbt.7.3.5364. Click
4 Sensitization of human melanoma cells by tamoxifen to apoptosis induction by pancratistatin, a nongenotoxic natural compound. Melanoma Res. 2011 Feb;21(1):1-11. doi: 10.1097/CMR.0b013e328337abff. Click
5 Narciclasine targets STAT3 via distinct mechanisms in tamoxifen-resistant breast cancer cells. Mol Ther Oncolytics. 2022 Jan 3;24:340-354. doi: 10.1016/j.omto.2021.12.025. Click
6 Combination of methylselenocysteine with tamoxifen inhibits MCF-7 breast cancer xenografts in nude mice through elevated apoptosis and reduced angiogenesis. Breast Cancer Res Treat. 2009 Nov;118(1):33-43. doi: 10.1007/s10549-008-0216-x. Click
7 The Combinatory Effects of Glabridin and Tamoxifen on Ishikawa and MCF-7 Cell Lines. Nat Prod Commun. 2015 Sep;10(9):1573-6. Click
8 Ginsenoside Rg3 overcomes tamoxifen resistance through inhibiting glycolysis in breast cancer cells. Cell Biol Int. 2024 Jan 15. doi: 10.1002/cbin.12123. Click
9 Evening Primrose Oil Enhances Tamoxifen's Anticancer Activity against Breast Cancer Cells by Inducing Apoptosis, Inhibiting Angiogenesis, and Arresting the Cell Cycle. Molecules. 2022 Apr 7;27(8):2391. doi: 10.3390/molecules27082391 Click
10 Celastrol enhances tamoxifen sensitivity in the treatment of triple negative breast cancer via mitochondria mediated apoptosis pathway. Am J Transl Res. 2023 Apr 15;15(4):2703-2715. Click
11 The Synergistic Effects of Celastrol in combination with Tamoxifen on Apoptosis and Autophagy in MCF-7 Cells. J Immunol Res. 2021 Jul 22;2021:5532269. doi: 10.1155/2021/5532269. Click
12 Carnosic acid cooperates with tamoxifen to induce apoptosis associated with Caspase-3 activation in breast cancer cells in vitro and in vivo. Biomed Pharmacother. 2017 May;89:827-837. doi: 10.1016/j.biopha.2017.01.084. Click
13 Enhancing Tamoxifen Therapy with α-Mangostin: Synergistic Antiproliferative Effects on Breast Cancer Cells and Potential Reduced Endometrial Impact. Pharmaceuticals (Basel). 2023 Nov 8;16(11):1576. doi: 10.3390/ph16111576. Click
14 Luteolin sensitises drug-resistant human breast cancer cells to tamoxifen via the inhibition of cyclin E2 expression. Food Chem. 2013 Nov 15;141(2):1553-61. doi: 10.1016/j.foodchem.2013.04.077. Click
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