General Information of Drug (ID: DM32FKD)

Drug Name
PF-228 Drug Info
Synonyms
869288-64-2; PF-573228; PF 573228; PF573228; PF-228; CHEMBL514554; 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone; 6-((4-((3-(Methylsulfonyl)benzyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-3,4-dihydroquinolin-2(1H)-one; 6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one; 6-[4-(3-Methanesulfonyl-benzylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-3,4-dihydro-1H-quinolin-2-one
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
11612883
ChEBI ID
CHEBI:91446
CAS Number
CAS 869288-64-2
TTD Drug ID
DM32FKD

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
Approved Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
VS-6063 DMGBLI3 Mesothelioma 2C51.2 Phase 2 [3]
BI-853520 DMNOSYW Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
PF-562271 DMSLE03 Solid tumour/cancer 2A00-2F9Z Phase 1 [5]
VS-4718 DMN9JCD Solid tumour/cancer 2A00-2F9Z Phase 1 [6]
GSK-2256098 DMR24MI Pulmonary arterial hypertension BB01.0 Phase 1 [7]
CEP-37440 DMV632P Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
IN10018 DMPXOVA Metastatic melanoma 2E2Z Phase 1 [8]
1,2,4-triazolo[1,5a]pyridine derivative 1 DMIUPSA N. A. N. A. Patented [9]
BMS-536924 DMXJB4N Discovery agent N.A. Investigative [10]
PMID23414845C30 DMNVQ29 Discovery agent N.A. Investigative [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [12]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [12]
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [14]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [15]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [16]
Oxazolyl methylthiothiazole derivative 1 DMZM6FW N. A. N. A. Patented [17]
PMID25991433-Compound-A1 DM89LF0 N. A. N. A. Patented [18]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [12]
Samuraciclib DM54FQA Breast cancer 2C60-2C65 Phase 1/2 [20]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [21]
BTX-A51 DMC8XHQ Advanced solid tumour 2A00-2F9Z Phase 1 [22]
SY-1365 DMK48PM Solid tumour/cancer 2A00-2F9Z Phase 1 [23]
LY3405105 DMB51K2 Solid tumour/cancer 2A00-2F9Z Phase 1 [24]
SY-5609 DMNW3LH Solid tumour/cancer 2A00-2F9Z Phase 1 [25]
Oxazolyl methylthiothiazole derivative 1 DMZM6FW N. A. N. A. Patented [17]
Roscovitine derivative 1 DMD1G3Z N. A. N. A. Patented [17]
Tricyclic benzimidazole derivative 1 DM5SD9E N. A. N. A. Patented [17]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [12]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
PHA848125 DMS2Q9G Thymic cancer 2C27 Phase 2 [26]
TG02 DMZFIGQ Anaplastic astrocytoma 2A00.0 Phase 1/2 [27]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [28]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [15]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [29]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [16]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMO-02 DMJRU3A Myotonic dystrophy 8C71.0 Phase 2/3 [30]
LY2090314 DMTBFE4 Acute myeloid leukaemia 2A60 Phase 2 [31]
Lithium DMZ3OU6 Bipolar disorder 6A60 Phase 2 [32]
Tideglusib DME4LA1 Alzheimer disease 8A20 Phase 2 [33]
9-ING-41 DM57TY3 Myelofibrosis 2A20.2 Phase 2 [34]
Neu-120 DMXKOUC Parkinson disease 8A00.0 Phase 1/2 [35]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [36]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [37]
TDZD-8 DMG6Q45 Malignant glioma 2A00.0 Patented [38]
AR-A014418 DMUPN01 Ovarian cancer 2C73 Patented [39]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [40]
Parthenolide DMCQBFT N. A. N. A. Phase 2 [41]
SAR-113945 DMMCA9V Osteoarthritis FA00-FA05 Phase 2 [42]
IMD-1041 DMU1MR9 Alzheimer disease 8A20 Phase 2 [43]
IMD-0354 DMOFSLE Acne vulgaris ED80 Phase 1 [44]
MLN0415 DMG72VK Arthritis FA20 Discontinued in Phase 1 [45]
5-Bromo-6-methoxy-9H-beta-carboline DM157OQ Discovery agent N.A. Investigative [46]
Staurosporine DM0E9BR Discovery agent N.A. Investigative [47]
5-amino-2-phenyl-oxazole-4-carboxylic acid amide DMX37ZC Discovery agent N.A. Investigative [48]
5-amino-2-p-tolyl-oxazole-4-carboxylic acid amide DM4SWJ7 Discovery agent N.A. Investigative [48]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Focal adhesion kinase 1 (PTK2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [49]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [50]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [51]
Quercetin DM3NC4M Obesity 5B81 Approved [52]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [53]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [54]
Testosterone DM7HUNW Hot flushes GA30 Approved [55]
Halothane DM80OZ5 Anaesthesia 9A78.6 Approved [56]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [57]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [58]
⏷ 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
Cyclin-dependent kinase 1 (CDK1) TTH6V3D CDK1_HUMAN Inhibitor [1]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [1]
Cyclin-dependent kinase 7 (CDK7) TTQYF7G CDK7_HUMAN Inhibitor [1]
Focal adhesion kinase 1 (FAK) TTON5IT FAK1_HUMAN Inhibitor [1]
Glycogen synthase kinase-3 beta (GSK-3B) TTRSMW9 GSK3B_HUMAN Inhibitor [1]
Inhibitor of nuclear factor kappa-B kinase beta (IKKB) TTJ3E9X IKKB_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Focal adhesion kinase 1 (PTK2) OT3Q1JDY FAK1_HUMAN Post-Translational Modifications [2]

References

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2 Aryl hydrocarbon receptor-dependent up-regulation of the heterodimeric amino acid transporter LAT1 (SLC7A5)/CD98hc (SLC3A2) by diesel exhaust particle extract in human bronchial epithelial cells. Toxicol Appl Pharmacol. 2016 Jan 1;290:74-85.
3 Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.
4 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
5 Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45.
6 FAK Inhibition disrupts a beta5 integrin signaling axis controlling anchorage-independent ovarian carcinoma growth. Mol Cancer Ther. 2014 Aug;13(8):2050-61.
7 A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Cell Cycle. 2014;13(19):3143-9.
8 Clinical pipeline report, company report or official report of InxMed.
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12 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
13 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.
14 P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther. 2007 Mar;6(3):926-34.
15 Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
16 A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected h... Cell Cycle. 2011 Mar 15;10(6):963-70.
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20 The CDK7 inhibitor CT7001 (Samuraciclib) targets proliferation pathways to inhibit advanced prostate cancer. Br J Cancer. 2023 Jun;128(12):2326-2337.
21 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
22 Clinical pipeline report, company report or official report of BioTheryX.
23 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
24 CDK7 inhibitors as anticancer drugs. Cancer Metastasis Rev. 2020 Sep;39(3):805-823.
25 Clinical pipeline report, company report or official report of Syros Pharmaceuticals.
26 Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.
27 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
28 ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
29 Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518.
30 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
31 Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015).Expert Opin Ther Pat. 2017 Jun;27(6):657-666.
32 The GSK3 kinase inhibitor lithium produces unexpected hyperphosphorylation of -catenin, a GSK3 substrate, in human glioblastoma cells. Biol Open. 2018 Jan 26;7(1):bio030874.
33 Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904.
34 9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer. Sci Rep. 2019 Dec 27;9(1):19977.
35 Company report (Neurim Pharmaceuticals)
36 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
37 Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
38 Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3beta inhibitors through virtual screening. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7232-6.
39 Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. Eur J Med Chem. 2009 Jun;44(6):2361-71.
40 How acute promyelocytic leukaemia revived arsenic. Nat Rev Cancer. 2002 Sep;2(9):705-13.
41 The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IkappaB kinase. Chem Biol. 2001 Aug;8(8):759-66.
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43 Inhibition of I B phosphorylation prevents load-induced cardiac dysfunction in mice. Am J Physiol Heart Circ Physiol. 2012 Dec 15;303(12):H1435-45.
44 I B kinase beta inhibitor IMD-0354 suppresses airway remodelling in a Dermatophagoides pteronyssinus-sensitized mouse model of chronic asthma. Clin Exp Allergy. 2011 Jan;41(1):104-15.
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47 UCN-01: a potent abrogator of G2 checkpoint function in cancer cells with disrupted p53. J Natl Cancer Inst. 1996 Jul 17;88(14):956-65.
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49 Estrogen and pure antiestrogen fulvestrant (ICI 182 780) augment cell-matrigel adhesion of MCF-7 breast cancer cells through a novel G protein coupled estrogen receptor (GPR30)-to-calpain signaling axis. Toxicol Appl Pharmacol. 2014 Mar 1;275(2):176-81. doi: 10.1016/j.taap.2014.01.005. Epub 2014 Jan 17.
50 Cleavage of focal adhesion kinase is an early marker and modulator of oxidative stress-induced apoptosis. Chem Biol Interact. 2008 Jan 10;171(1):57-66. doi: 10.1016/j.cbi.2007.08.009. Epub 2007 Aug 19.
51 Simvastatin inactivates beta1-integrin and extracellular signal-related kinase signaling and inhibits cell proliferation in head and neck squamous cell carcinoma cells. Cancer Sci. 2007 Jun;98(6):890-9.
52 Quercetin inhibits migration and invasion of SAS human oral cancer cells through inhibition of NF-B and matrix metalloproteinase-2/-9 signaling pathways. Anticancer Res. 2013 May;33(5):1941-50.
53 Effect of all-trans retinoic acid on sodium/iodide symporter expression, radioiodine uptake and gene expression profiles in a human anaplastic thyroid carcinoma cell line. Nucl Med Biol. 2006 Oct;33(7):875-82. doi: 10.1016/j.nucmedbio.2006.07.004.
54 Activation of cannabinoid receptors promote periodontal cell adhesion and migration. J Clin Periodontol. 2019 Dec;46(12):1264-1272. doi: 10.1111/jcpe.13190. Epub 2019 Oct 22.
55 Monomeric and oligomeric flavanols are agonists of membrane androgen receptors. Exp Cell Res. 2005 Oct 1;309(2):329-39. doi: 10.1016/j.yexcr.2005.06.011.
56 Disruption of FAK signaling: a side mechanism in cytotoxicity. Toxicology. 2008 Mar 12;245(1-2):1-10. doi: 10.1016/j.tox.2007.12.003. Epub 2007 Dec 15.
57 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
58 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.