Identification
- Summary
Bosutinib is an antineoplastic agent used for the treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) in adults with inadequate clinical response to other treatments.
- Brand Names
- Bosulif
- Generic Name
- Bosutinib
- DrugBank Accession Number
- DB06616
- Background
Bosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Bosutinib (DB06616)
- Weight
- Average: 530.446
Monoisotopic: 529.164745233 - Chemical Formula
- C26H29Cl2N5O3
- Synonyms
- 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile
- Bosutinib
- External IDs
- SK-606
- SKI 606
- SKI-606
Pharmacology
- Indication
Treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy in adult patients.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Not Available
- Mechanism of action
Bosutinib is a tyrosine kinase inhibitor. Although it is able to inhibit several tyrosine kinases such as Src, Lyn, and Hck, which are members of the Src-family of kinases, its primary target is the Bcr-Abl kinase. The Bcr-Abl gene is a chimeric oncogene created from the fusion of the breakpoint-cluster (Bcr) gene and Abelson (Abl) tyrosine gene. This chromosomal abnormality results in the formation of what is commonly known as the Philadelphia chromosome or Philadelphia translocation. The Bcr-Abl gene expresses a particular kinase that promotes the progression of CML. A decrease in the growth and size of the CML tumour has been observed following administration of bosutinib. Bosutinib did not inhibit the T315I and V299L mutant cells.
Target Actions Organism ABreakpoint cluster region protein inhibitorHumans ATyrosine-protein kinase ABL1 inhibitorHumans UTyrosine-protein kinase Lyn Not Available Humans UTyrosine-protein kinase HCK inhibitorHumans UProto-oncogene tyrosine-protein kinase Src inhibitorHumans UCyclin-dependent kinase 2 inhibitorHumans UDual specificity mitogen-activated protein kinase kinase 1 inhibitorHumans UDual specificity mitogen-activated protein kinase kinase 2 inhibitorHumans UMitogen-activated protein kinase kinase kinase 2 inhibitorHumans UCalcium/calmodulin-dependent protein kinase type II subunit gamma inhibitorHumans - Absorption
Food increase the exposure of bosutinib. Tmax, single dose, cancer patients, fed-state = 4-6 hours; After 15 daily doses of bosutinib 500 mg with food in CML patients, the pharmacokinetic parameters are as follows: Cmax = 200 ng/mL; AUC = 3650 ng∙h/mL
- Volume of distribution
Apparent volume of distribution = 6080 ± 1230 L.
- Protein binding
94% bound to human plasma proteins in vitro. 96% bound to human plasma proteins in healthy subjects ex vivo. Extent of protein binding is not concentration-dependent.
- Metabolism
Bosutinib is primarily metabolized by CYP3A4. The major circulating metabolites identified in plasma are oxydechlorinated (M2) bosutinib (19% of parent exposure) and N-desmethylated (M5) bosutinib (25% of parent exposure), with bosutinib N-oxide (M6) as a minor circulating metabolite. All the metabolites were deemed inactive.
- Route of elimination
When given a single oral dose, 91.3% of the dose was recovered in feces and 3% of the dose recovered in urine.
- Half-life
Terminal phase elimination half-life, single oral dose, fed-state = 22.5 hours
- Clearance
Mean clearance (CL/F), single oral dose, fed-state = 189 L/h
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Most common adverse reactions (incidence greater than 20%) are diarrhea, nausea, thrombocytopenia, vomiting, abdominal pain, rash, anemia, pyrexia, and fatigue. Because bosutinib is not an inhibitor of c-KIT or PDGF receptor, it has less hematologic toxicities.
- Pathways
Pathway Category Bosutinib Inhibition of BCR-ABL Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Bosutinib. Abametapir The serum concentration of Bosutinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Bosutinib can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Bosutinib. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Bosutinib. Abrocitinib The serum concentration of Bosutinib can be increased when it is combined with Abrocitinib. Acalabrutinib The metabolism of Bosutinib can be decreased when combined with Acalabrutinib. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Bosutinib. Acetaminophen The metabolism of Bosutinib can be increased when combined with Acetaminophen. Acetazolamide The metabolism of Bosutinib can be decreased when combined with Acetazolamide. 
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- Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of bosutinib.
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of bosutinib.
- Take with food. Coadministration with a high-fat meal may increase the AUC of bosutinib.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Bosutinib monohydrate 844ZJE6I55 918639-08-4 BXPOSPOKHGNMEP-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bosulif Tablet, film coated 500 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU 
Bosulif Tablet 400 mg Oral Pfizer Canada Ulc Not applicable Not applicable Canada 
Bosulif Tablet, film coated 400 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2017-12-18 Not applicable US 
Bosulif Tablet, film coated 100 mg/1 Oral U.S. Pharmaceuticals 2012-09-04 Not applicable US Bosulif Tablet, film coated 100 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU Bosulif Tablet, film coated 100 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU Bosulif Tablet 500 mg Oral Pfizer Canada Ulc 2014-03-24 Not applicable Canada Bosulif Tablet, film coated 500 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2012-09-04 Not applicable US Bosulif Tablet, film coated 400 mg Oral Pfizer Europe Ma Eeig 2020-12-16 Not applicable EU Bosulif Tablet, film coated 500 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU
Categories
- ATC Codes
- L01XE14 — Bosutinib
- Drug Categories
- Amines
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Heterocyclic Compounds, Fused-Ring
- Immunosuppressive Agents
- Kinase Inhibitor
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Protein Kinase Inhibitors
- Tyrosine Kinase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 4-aminoquinolines. These are organic compounds containing an amino group attached to the 4-position of a quinoline ring system.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Aminoquinolines and derivatives
- Direct Parent
- 4-aminoquinolines
- Alternative Parents
- Aminophenyl ethers / Methoxyanilines / Phenoxy compounds / Anisoles / Dichlorobenzenes / Methoxybenzenes / Alkyl aryl ethers / Aminopyridines and derivatives / N-methylpiperazines / Aryl chlorides show 8 more
- Substituents
- 1,3-dichlorobenzene / 1,4-diazinane / 4-aminoquinoline / Alkyl aryl ether / Amine / Aminophenyl ether / Aminopyridine / Aniline or substituted anilines / Anisole / Aromatic heteropolycyclic compound show 30 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, aromatic ether, nitrile, dichlorobenzene, aminoquinoline, N-methylpiperazine (CHEBI:39112)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 5018V4AEZ0
- CAS number
- 380843-75-4
- InChI Key
- UBPYILGKFZZVDX-UHFFFAOYSA-N
- InChI
- InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)
- IUPAC Name
- 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
- SMILES
- COC1=CC(NC2=C(C=NC3=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23)C#N)=C(Cl)C=C1Cl
References
- General References
- Amsberg GK, Schafhausen P: Bosutinib in the management of chronic myelogenous leukemia. Biologics. 2013;7:115-22. doi: 10.2147/BTT.S30182. Epub 2013 May 6. [Article]
- Keller-V Amsberg G, Brummendorf TH: Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia. Expert Rev Anticancer Ther. 2012 Sep;12(9):1121-7. doi: 10.1586/era.12.84. [Article]
- External Links
- Human Metabolome Database
- HMDB0240205
- KEGG Drug
- D03252
- PubChem Compound
- 5328940
- PubChem Substance
- 175427079
- ChemSpider
- 4486102
- BindingDB
- 4552
- 1307619
- ChEBI
- 39112
- ChEMBL
- CHEMBL288441
- ZINC
- ZINC000022448983
- PDBe Ligand
- DB8
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Bosutinib
- PDB Entries
- 3soa / 3ue4 / 4mxo / 4mxx / 4mxy / 4mxz / 4qmn / 5ajq / 5i9x / 5vc3 … show 3 more
- FDA label
- Download (326 KB)
- MSDS
- Download (97.1 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Acute Lymphoblastic Leukemia (ALL) / Leukemia Chronic Myelogenous Leukemia (CML) 1 4 Terminated Treatment Previously Treated PH + CML 1 3 Active Not Recruiting Treatment Leukemia Chronic Myelogenous Leukemia (CML) 1 3 Completed Treatment Chronic Myeloid Leukemia (CML) 1 3 Completed Treatment Leukemia, Myelogenous, Chronic, Breakpoint Cluster Region-Abelson Proto-oncogene (BCR-ABL) Positive 1 3 Recruiting Treatment Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) 1 2 Active Not Recruiting Treatment Chronic Myeloid Leukemia (CML) 1 2 Active Not Recruiting Treatment Chronic Myeloid Leukemia (CML) / Chronic Myeloid Leukemia in Remission / Leukemia, Myelogenous, Chronic, BCR-ABL Positive 1 2 Completed Treatment Autosomal Dominant Polycystic Kidney Disease （ADPKD) 1 2 Completed Treatment BCR-ABL Positive / Chronic / Leukemias / Myelogenous 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 100 mg Tablet Oral 400 mg Tablet Oral 500 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 100 MG Tablet, film coated Oral 400 mg/1 Tablet, film coated Oral 400 MG Tablet, film coated Oral 500 mg/1 Tablet, film coated Oral 500 MG Tablet, film coated Oral Tablet, coated Oral 500 mg Tablet, coated Oral 100 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6002008 No 1999-12-14 2018-03-27 US US7417148 No 2008-08-26 2026-01-23 US USRE42376 No 2011-05-17 2019-09-24 US US7767678 No 2010-08-03 2026-11-23 US US7919625 No 2011-04-05 2025-12-11 US US11103497 No 2014-02-28 2034-02-28 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0095 mg/mL ALOGPS logP 4.87 ALOGPS logP 4.09 ChemAxon logS -4.8 ALOGPS pKa (Strongest Acidic) 15.48 ChemAxon pKa (Strongest Basic) 8.03 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 82.88 Å2 ChemAxon Rotatable Bond Count 9 ChemAxon Refractivity 142.12 m3·mol-1 ChemAxon Polarizability 56.02 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9823 Blood Brain Barrier + 0.9272 Caco-2 permeable + 0.6542 P-glycoprotein substrate Substrate 0.7601 P-glycoprotein inhibitor I Inhibitor 0.8409 P-glycoprotein inhibitor II Inhibitor 0.9108 Renal organic cation transporter Inhibitor 0.5663 CYP450 2C9 substrate Non-substrate 0.854 CYP450 2D6 substrate Non-substrate 0.6953 CYP450 3A4 substrate Substrate 0.6987 CYP450 1A2 substrate Inhibitor 0.5606 CYP450 2C9 inhibitor Non-inhibitor 0.7372 CYP450 2D6 inhibitor Non-inhibitor 0.5136 CYP450 2C19 inhibitor Non-inhibitor 0.5725 CYP450 3A4 inhibitor Inhibitor 0.5 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7021 Ames test AMES toxic 0.5922 Carcinogenicity Non-carcinogens 0.8869 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.4201 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.6147 hERG inhibition (predictor II) Inhibitor 0.7754
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-014i-0092000000-68183c460c3cf8e08c01 MS/MS Spectrum - , positive LC-MS/MS splash10-001l-1900080000-86f44693fc4098040447
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Rho guanyl-nucleotide exchange factor activity
- Specific Function
- GTPase-activating protein for RAC1 and CDC42. Promotes the exchange of RAC or CDC42-bound GDP by GTP, thereby activating them. Displays serine/threonine kinase activity.
- Gene Name
- BCR
- Uniprot ID
- P11274
- Uniprot Name
- Breakpoint cluster region protein
- Molecular Weight
- 142818.07 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Syntaxin binding
- Specific Function
- Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility a...
- Gene Name
- ABL1
- Uniprot ID
- P00519
- Uniprot Name
- Tyrosine-protein kinase ABL1
- Molecular Weight
- 122871.435 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Receptor signaling protein tyrosine kinase activity
- Specific Function
- Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, respons...
- Gene Name
- LYN
- Uniprot ID
- P07948
- Uniprot Name
- Tyrosine-protein kinase Lyn
- Molecular Weight
- 58573.595 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Receptor binding
- Specific Function
- Non-receptor tyrosine-protein kinase found in hematopoietic cells that transmits signals from cell surface receptors and plays an important role in the regulation of innate immune responses, includ...
- Gene Name
- HCK
- Uniprot ID
- P08631
- Uniprot Name
- Tyrosine-protein kinase HCK
- Molecular Weight
- 59599.355 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sh3/sh2 adaptor activity
- Specific Function
- Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion recept...
- Gene Name
- SRC
- Uniprot ID
- P12931
- Uniprot Name
- Proto-oncogene tyrosine-protein kinase Src
- Molecular Weight
- 59834.295 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, N...
- Gene Name
- CDK2
- Uniprot ID
- P24941
- Uniprot Name
- Cyclin-dependent kinase 2
- Molecular Weight
- 33929.215 Da
References
- Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Receptor signaling protein tyrosine phosphatase activity
- Specific Function
- Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones t...
- Gene Name
- MAP2K1
- Uniprot ID
- Q02750
- Uniprot Name
- Dual specificity mitogen-activated protein kinase kinase 1
- Molecular Weight
- 43438.65 Da
References
- Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Scaffold protein binding
- Specific Function
- Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity).
- Gene Name
- MAP2K2
- Uniprot ID
- P36507
- Uniprot Name
- Dual specificity mitogen-activated protein kinase kinase 2
- Molecular Weight
- 44423.735 Da
References
- Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Protein serine/threonine kinase activity
- Specific Function
- Component of a protein kinase signal transduction cascade. Regulates the JNK and ERK5 pathways by phosphorylating and activating MAP2K5 and MAP2K7 (By similarity). Plays a role in caveolae kiss-and...
- Gene Name
- MAP3K2
- Uniprot ID
- Q9Y2U5
- Uniprot Name
- Mitogen-activated protein kinase kinase kinase 2
- Molecular Weight
- 69740.21 Da
References
- Ahmad S, Hughes MA, Johnson GL, Scott JE: Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors. J Biomol Screen. 2013 Apr;18(4):388-99. doi: 10.1177/1087057112466430. Epub 2012 Nov 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Protein homodimerization activity
- Specific Function
- Calcium/calmodulin-dependent protein kinase that functions autonomously after Ca(2+)/calmodulin-binding and autophosphorylation, and is involved in sarcoplsamic reticulum Ca(2+) transport in skelet...
- Gene Name
- CAMK2G
- Uniprot ID
- Q13555
- Uniprot Name
- Calcium/calmodulin-dependent protein kinase type II subunit gamma
- Molecular Weight
- 62608.655 Da
References
- Amsberg GK, Koschmieder S: Profile of bosutinib and its clinical potential in the treatment of chronic myeloid leukemia. Onco Targets Ther. 2013;6:99-106. doi: 10.2147/OTT.S19901. Epub 2013 Mar 4. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Filppula AM, Neuvonen PJ, Backman JT: In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9. doi: 10.1124/dmd.114.057695. Epub 2014 Apr 8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Filppula AM, Neuvonen PJ, Backman JT: In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9. doi: 10.1124/dmd.114.057695. Epub 2014 Apr 8. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
Drug created at March 19, 2008 16:41 / Updated at May 22, 2022 04:54