General Information of Drug (ID: DMPK32V)

Drug Name
BMS-754807 Drug Info
Synonyms
BMS-754807; 1001350-96-4; BMS 754807; BMS754807; UNII-W9E3353E8J; CHEMBL575448; CHEBI:88339; W9E3353E8J; 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-prolinamide; W-204348; J-501009; 2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-, (2S)-;2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridin
Cross-matching ID
PubChem CID
24785538
ChEBI ID
CHEBI:88339
CAS Number
CAS 1001350-96-4
TTD Drug ID
DMPK32V

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [3]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [3]
GDC-0068 DMWBZJD Breast cancer 2C60-2C65 Phase 3 [3]
CI-1033 DMSI8N3 Lymphoma 2A80-2A86 Phase 2 [4]
CMX-2043 DMPSCVY Cardiac disease BA00-BE2Z Phase 2 [5]
ARQ 092 DM5WK0J Proteus syndrome LD2C Phase 2 [6]
GSK2110183 DMZHB37 leukaemia 2A60-2B33 Phase 2 [7]
RX-0201 DMTBAV3 Pancreatic cancer 2C10 Phase 2 [8]
PTX-200 DM0ZIT2 Breast cancer 2C60-2C65 Phase 2 [3]
Triciribine prodrug DMBN1XS Solid tumour/cancer 2A00-2F9Z Phase 1/2 [7]
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [9]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [10]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [11]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [12]
Gefitinib DM15F0X Colon adenocarcinoma Approved [13]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [14]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [15]
Selenium DM25CGV N. A. N. A. Approved [16]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [17]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [18]
⏷ Show the Full List of 20 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [19]
Gefitinib DM15F0X Colon adenocarcinoma Approved [20]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [17]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [21]
Quercetin DM3NC4M Obesity 5B81 Approved [22]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [23]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [24]
Testosterone DM7HUNW Hot flushes GA30 Approved [25]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [25]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [27]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [28]
Gefitinib DM15F0X Colon adenocarcinoma Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [14]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [30]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [32]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [33]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [34]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [35]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [36]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [37]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [12]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [38]
Gefitinib DM15F0X Colon adenocarcinoma Approved [39]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [40]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [41]
Selenium DM25CGV N. A. N. A. Approved [16]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [18]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [43]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [44]
Prednisone DM2HG4X Acute asthma CA23 Approved [45]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [46]
Quercetin DM3NC4M Obesity 5B81 Approved [47]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [48]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [49]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [50]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [51]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [52]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [53]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [54]
Gefitinib DM15F0X Colon adenocarcinoma Approved [55]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [40]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [56]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [30]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [57]
Methotrexate DM2TEOL Anterior urethra cancer Approved [58]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [59]
Quercetin DM3NC4M Obesity 5B81 Approved [60]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
RAC-alpha serine/threonine-protein kinase (AKT1) TTWTSCV AKT1_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cyclin-dependent kinase inhibitor 2A (CDKN2A) OTN0ZWAE CDN2A_HUMAN Drug Response [2]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Drug Response [2]
Insulin-like growth factor 1 receptor (IGF1R) OTXJIF13 IGF1R_HUMAN Post-Translational Modifications [2]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Post-Translational Modifications [2]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Drug Response [2]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Post-Translational Modifications [2]

References

1 Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in cli... J Med Chem. 2009 Dec 10;52(23):7360-3.
2 CDK4/6 and IGF1 receptor inhibitors synergize to suppress the growth of p16INK4A-deficient pancreatic cancers. Cancer Res. 2014 Jul 15;74(14):3947-58. doi: 10.1158/0008-5472.CAN-13-2923. Epub 2014 Jul 1.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
5 Pre-clinical and Clinical Safety Studies of CMX-2043: a cytoprotective lipoic acid analogue for ischaemia-reperfusion injury. Basic Clin Pharmacol Toxicol. 2014 Nov;115(5):456-64.
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1479).
8 CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
9 Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
10 Nicotine-induced survival signaling in lung cancer cells is dependent on their p53 status while its down-regulation by curcumin is independent. Mol Cancer. 2010 Aug 20;9:220.
11 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
12 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
13 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
14 Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
15 Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2015 Mar;35(3):1063-76. doi: 10.1111/liv.12626. Epub 2014 Jul 30.
16 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
17 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
18 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
19 Estrogen utilization of IGF-1-R and EGF-R to signal in breast cancer cells. J Steroid Biochem Mol Biol. 2010 Feb 28;118(4-5):219-30. doi: 10.1016/j.jsbmb.2009.09.018. Epub 2009 Oct 6.
20 Implication of the insulin-like growth factor-IR pathway in the resistance of non-small cell lung cancer cells to treatment with gefitinib. Clin Cancer Res. 2007 May 1;13(9):2795-803. doi: 10.1158/1078-0432.CCR-06-2077.
21 Simvastatin inhibits the proliferation of human prostate cancer PC-3 cells via down-regulation of the insulin-like growth factor 1 receptor. Biochem Biophys Res Commun. 2008 Jul 25;372(2):356-61. doi: 10.1016/j.bbrc.2008.05.043. Epub 2008 May 19.
22 Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
23 Arsenic trioxide and cisplatin synergism increase cytotoxicity in human ovarian cancer cells: therapeutic potential for ovarian cancer. Cancer Sci. 2009 Dec;100(12):2459-64.
24 Delta9-tetrahydrocannabinol inhibits cytotrophoblast cell proliferation and modulates gene transcription. Mol Hum Reprod. 2006 May;12(5):321-33. doi: 10.1093/molehr/gal036. Epub 2006 Apr 5.
25 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
26 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
27 Rapamycin sensitizes multiple myeloma cells to apoptosis induced by dexamethasone. Blood. 2004 Apr 15;103(8):3138-47. doi: 10.1182/blood-2003-05-1543. Epub 2003 Dec 24.
28 Antidepressant drug sertraline modulates AMPK-MTOR signaling-mediated autophagy via targeting mitochondrial VDAC1 protein. Autophagy. 2021 Oct;17(10):2783-2799. doi: 10.1080/15548627.2020.1841953. Epub 2020 Nov 9.
29 EGFR tyrosine kinase inhibitors activate autophagy as a cytoprotective response in human lung cancer cells. PLoS One. 2011;6(6):e18691. doi: 10.1371/journal.pone.0018691. Epub 2011 Jun 2.
30 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
31 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
32 SU5416 inhibited VEGF and HIF-1alpha expression through the PI3K/AKT/p70S6K1 signaling pathway. Biochem Biophys Res Commun. 2004 Nov 12;324(2):471-80. doi: 10.1016/j.bbrc.2004.09.082.
33 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
34 D-glucosamine down-regulates HIF-1alpha through inhibition of protein translation in DU145 prostate cancer cells. Biochem Biophys Res Commun. 2009 Apr 24;382(1):96-101. doi: 10.1016/j.bbrc.2009.02.129. Epub 2009 Feb 28.
35 Arsenic trioxide inhibits translation of mRNA of bcr-abl, resulting in attenuation of Bcr-Abl levels and apoptosis of human leukemia cells. Cancer Res. 2003 Nov 15;63(22):7950-8.
36 The nonsteroidal anti-inflammatory drugs aspirin and indomethacin attenuate beta-catenin/TCF-4 signaling. Oncogene. 2001 Feb 1;20(5):645-53. doi: 10.1038/sj.onc.1204123.
37 Novel mechanism of cannabidiol-induced apoptosis in breast cancer cell lines. Breast. 2018 Oct;41:34-41. doi: 10.1016/j.breast.2018.06.009. Epub 2018 Jun 22.
38 Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens. Toxicol Appl Pharmacol. 2010 Jun 1;245(2):160-70. doi: 10.1016/j.taap.2010.02.015. Epub 2010 Mar 4.
39 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
40 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
41 Resveratrol attenuates senescence of adipose-derived mesenchymal stem cells and restores their paracrine effects on promoting insulin secretion of INS-1 cells through Pim-1. Eur Rev Med Pharmacol Sci. 2016;20(6):1203-13.
42 Cell cycle effects of nonsteroidal anti-inflammatory drugs and enhanced growth inhibition in combination with gemcitabine in pancreatic carcinoma cells. J Pharmacol Exp Ther. 2001 Sep;298(3):976-85.
43 Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
44 Minimal peroxide exposure of neuronal cells induces multifaceted adaptive responses. PLoS One. 2010 Dec 17;5(12):e14352. doi: 10.1371/journal.pone.0014352.
45 Glucocorticoids induce G1 arrest of lymphoblastic cells through retinoblastoma protein Rb1 dephosphorylation in childhood acute lymphoblastic leukemia in vivo. Cancer Biol Ther. 2004 May;3(5):470-6. doi: 10.4161/cbt.3.5.838. Epub 2004 May 9.
46 A gene signature-based approach identifies thioridazine as an inhibitor of phosphatidylinositol-3'-kinase (PI3K)/AKT pathway in ovarian cancer cells. Gynecol Oncol. 2011 Jan;120(1):121-7. doi: 10.1016/j.ygyno.2010.10.003. Epub 2010 Oct 29.
47 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
48 Expression of the helix-loop-helix protein inhibitor of DNA binding-1 (ID-1) is activated by all-trans retinoic acid in normal human keratinocytes. Toxicol Appl Pharmacol. 2006 Aug 1;214(3):219-29. doi: 10.1016/j.taap.2005.12.015. Epub 2006 Feb 21.
49 Azidothymidine and cisplatin increase p14ARF expression in OVCAR-3 ovarian cancer cell line. Toxicol Appl Pharmacol. 2006 Oct 1;216(1):89-97. doi: 10.1016/j.taap.2006.04.015. Epub 2006 May 19.
50 [Re-expression of p16 gene in myeloma cell line U266 by arsenic trioxide]. Ai Zheng. 2004 Jun;23(6):626-30.
51 p16 loss facilitate hydroquinone-induced malignant transformation of TK6 cells through promoting cell proliferation and accelerating the cell cycle progression. Environ Toxicol. 2021 Aug;36(8):1591-1599. doi: 10.1002/tox.23155. Epub 2021 May 1.
52 Delta 9-tetrahydrocannabinol inhibits cell cycle progression by downregulation of E2F1 in human glioblastoma multiforme cells. Acta Oncol. 2008;47(6):1062-70.
53 Indomethacin inhibits cell growth of medullary thyroid carcinoma by reducing cell cycle progression into S phase. Exp Biol Med (Maywood). 2008 Nov;233(11):1433-40. doi: 10.3181/0804-RM-127. Epub 2008 Sep 12.
54 Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer. 2011 Apr 28;18(3):333-45. doi: 10.1530/ERC-10-0262. Print 2011 Jun.
55 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
56 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
57 Sulindac induces specific degradation of the HPV oncoprotein E7 and causes growth arrest and apoptosis in cervical carcinoma cells. Cancer Lett. 2007 Jan 8;245(1-2):103-11. doi: 10.1016/j.canlet.2005.12.034. Epub 2006 Feb 20.
58 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
59 HMG-CoA reductase inhibitor simvastatin inhibits cell cycle progression at the G1/S checkpoint in immortalized lymphocytes from Alzheimer's disease patients independently of cholesterol-lowering effects. J Pharmacol Exp Ther. 2008 Jan;324(1):352-9. doi: 10.1124/jpet.107.128959. Epub 2007 Oct 10.
60 Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.