General
Preferred name
PONATINIB
Synonyms
AP-24534 ()
KIN001-192 ()
AP-24534 HCl, AP-24534, Iclusig, Ponatinib HCl ()
AP24534 ()
AP24534 Hydrochloride ()
AP 24534 ()
AP-24534 Hydrochloride ()
PONATINIB HYDROCHLORIDE ()
AP24534 (Ponatinib) ()
PMID25656651-Compound-5 ()
Ponatinib (hydrochloride) ()
AP24534 (hydrochloride) ()
Ponatinib (AP24534) ()
PonatinibAP24534S1490A3349Benzamide, 3-(2-imidazo[1,2-b]-pyridazin-3-ylethynyl)-4-methyl-N-[4[(4-methyl-1-piperazinyl)-methyl]-3-(trifluoromethyl)-phenyl]- ()
ICLUSIG ()
AP-24534 HCl ()
AP24534 HCL ()
Ponatinib-d8 ()
Ponatinib (hydroachloride) ()
P&D ID
PD004100
CAS
943319-70-8
1114544-31-8
1562993-37-6
Tags
available
covalent binder
drug
Approved by
FDA
First approval
2012
Drug indication
Acute lymphoblastic leukaemia
chronic myelogenous leukemia
Chronic myeloid leukaemia
Neoplasm
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Ponatinib is a Type-1 kinase inhibitor. It is a thrid generation BCR-Abl inhibitor. Use of ponatinib is subject to additional monitoring due to the observed serious risk of liver problems or blood clots (including heart attack and stroke).
Marketed formulations contain ponatinib hydrochloride (PubChem CID 46908927).
DESCRIPTION Ponatinib is a Type-1 kinase inhibitor. It is a thrid generation BCR-Abl inhibitor. Use of ponatinib is subject to additional monitoring due to the observed serious risk of liver problems or blood clots (including heart attack and stroke, collectively referred to as arterial occlusive events, or AOEs). Final 5-year results of safety and efficacy in Ph+ leukemia as evaluated in NCT01207440 are reported by Cortes et al. (2018) .
Marketed formulations contain ponatinib hydrochloride (PubChem CID 46908927).
ABSORPTION The absolute bioavailability of ponatinib is unknown. Peak concentrations of ponatinib are observed within 6 hours after Iclusig oral administration. Food does not affect absorption of food. The aqueous solubility of ponatinib is pH dependent, with higher pH resulting in lower solubility.; When 45 mg of ponatinib is given to cancer patients, the pharmacokinetic parameters are as follows: ; Cmax = 73 ng/mL;; AUC = 1253 ng•hr/mL;
DESCRIPTION Ponatinib is a Type-1 kinase inhibitor. It is a third generation BCR-Abl inhibitor. Use of ponatinib is subject to additional monitoring due to the observed serious risk of liver problems or blood clots (including heart attack and stroke, collectively referred to as arterial occlusive events, or AOEs). Final 5-year results of safety and efficacy in Ph+ leukemia as evaluated in NCT01207440 are reported by Cortes et al. (2018) .
Marketed formulations contain ponatinib hydrochloride (PubChem CID 46908927).
Ponatinib has also been reported as a dual inhibitor of RIPK1 and RIPK3 which inhibits experimental models of RIPK1- and RIPK3-dependent cell death (necroptosis) . On the basis of these findings, hybrid ponatinib/ (a RIPK1 and IDO inhibitor) were designed and tested for potential to target RIPK1- and RIPK3-driven inflammatory pathologies. (GtoPdb)
DESCRIPTION Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFR¦Á, VEGFR2, FGFR1, and Src, respectively[1].
PRICE 50
DESCRIPTION Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFR??), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).
DESCRIPTION Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFR¦Á, VEGFR2, FGFR1, and Src, respectively[1].
PRICE 42
DESCRIPTION Ponatinib Hydrochloride (AP-24534 Hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFR??, VEGFR2, FGFR1, and Src, respectively.
DESCRIPTION Ponatinib is indicated for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy. (PKIDB)
DESCRIPTION Selective Chk1 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Ponatinib is a kinase inhibitor used to treat patients with various types of chronic myeloid leukemia (CML). (Enamine Bioactive Compounds)
DESCRIPTION Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src). (TargetMol Bioactive Compound Library)
DESCRIPTION Ponatinib Hydrochloride (AP-24534 Hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively. (TargetMol Bioactive Compound Library)
Cell lines
659
Organisms
0
Compound Sets
38
AdooQ Bioactive Compound Library
A10080
Axon Medchem Screening Library
1857
Cayman Chemical Bioactives
11494
35778
28905
ChEMBL Approved Drugs
CHEMBL1171837
CHEMBL2105708
ChEMBL Drugs
CHEMBL1171837
CHEMBL2105708
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5890
Concise Guide to Pharmacology 2019/20
5890
Concise Guide to Pharmacology 2021/22
5890
Concise Guide to Pharmacology 2023/24
5890
CovalentInDB
CI007241
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08901
DrugBank Approved Drugs
DB08901
DrugCentral
4716
DrugCentral Approved Drugs
4716
DrugMAP
DMAI95U
DMYGJQO
DrugMAP Approved Drugs
DMYGJQO
Enamine Bioactive Compounds
EBC-11436
EU-OPENSCREEN Bioactive Compound Library
EOS100606
Guide to Pharmacology
5890
JUMP-MOA Compound Set
24826799
JUMP-Target 1 Compound Set
24826799
LINCS compound set
10150-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1171837
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1171837
MedChem Express Bioactive Compound Library
HY-12047
HY-108766
NCATS Inxight Approved Drugs
4340891KFS
NIH Approved Oncology Drugs
440800632
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
AP24534
TargetMol Bioactive Compound Library
T2372
T2372L
Tocris Bioactive Compound Library
4274
Welcome Trust Cancer Drugs
155
ZINC Tool Compounds
ZINC000036701290
External IDs
61
Properties
(calculated by RDKit )
Molecular Weight
532.22
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
4
cLogP
4.46
TPSA
65.77
Fraction CSP3
0.28
Chiral centers
0.0
Largest ring
6.0
QED
0.39
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Autophagy
Bcr-Abl
FGFR
PDGFR
SRC
VEGFR
ABL
PDGFRα
VEGFR2
FGFR1
ABL1, BCR, FGFR1, FGFR2, FGFR3, FGFR4, FLT3, KDR, KIT, LCK, LYN, PDGFRA, RET, SRC, TEK
Bcr-Abl inhibitor
Lyn
Autophagy,Bcr-Abl,FGFR,PDGFR,Src,VEGFR
BCR
KIT
RET
TEK
FLT3
FGFR2
FGFR3
FGFR4
LCK
KDR
PDGFRA
c-Src
Pathway
ABL signaling
Angiogenesis
Cytoskeletal Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Targets
ABL1
Primary Target
Abl Kinase
MOA
c-Kit
Src
Inhibitor
Inhibitors of Signal Transduction Pathways
Bcr-Abl Kinase Inhibitors
Bcr-Abl kinase inhibitor, FLT3 inhibitor, PDGFR tyrosine kinase receptor inhibitor
Bcr-Abl kinase inhibitor
Member status
virtual
Indication
chronic myeloid leukemia (CML), acute lymphoblastic leukemia (ALL)
Source data