General
Preferred name
QUIZARTINIB
Synonyms
AC220 ()
QUIZARTINIB DIHYDROCHLORIDE ()
AC220, AC-220, Quizartinib Dihydrochloride, AC010220.2HCl, AC010220, ASP-2689 ()
AC220 (Quizartinib) ()
AC 220 dihydrochloride ()
AC 220 ()
Quizartinib (dihydrochloride) ()
AC708 ()
AC220 (dihydrochloride) ()
Quizartinib (AC220) ()
AC-010220 ()
AC-220 ()
AC010220 ()
ASP-2689 ()
AC010220.2HCl ()
Quizartinib monohydrochloride ()
AC220 2HCL ()
AC-220 DIHYDROCHLORIDE ()
Quizartinib hydrochloride ()
AC010220 2HCL ()
AC-010220 DIHYDROCHLORIDE ()
Vanflyta ()
P&D ID
PD003221
CAS
950769-58-1
1132827-21-4
Tags
available
probe
PROTAC
drug
Approved by
PMDA
FDA
First approval
2019
2023
Drug indication
Acute myeloid leukaemia
leukaemia
Acute myeloid leukemia
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
experimental probe
calculated probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Tool Compound Set
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT No nonhuman ortholog potencies were reported. Acute oral dosing in mice was shown be tolerated (up to 300 mg/kg), though PK was linear up through 100 mg/kg. Repeat dosing was only performed at 10 mg/kg. RET, PDGFRA, PDGFRB, CSF1R are the only kinases within 10x. The recommended upper in vitro concentration is intended to minimize off-target RTK activity. Jun 10 2016 - 4:13am; AC220 is potent and selective and has good PK characteristics. While activity in certain biochemical assays and cellular assays may be evident as low as 0.1-10 nM, drug-resistant models may require concentrations as high as 100-300 nM. It has been compared with and/or combined with other anticancer agents such as G-749 (FLT3 inhibitor) and JQ1 (BET protein antagonist) in various models, with resistant AML being an initial disease target in humans. Jun 10 2016 - 4:14am; This probe has a number of targets other than FLT3 and is active at 300 nM in human primary cell assays that do not express FLT3. If used as a target-selective probe in a study, this data should be supplemented by target knock-down and over expression of a constitutively active form to confirm involvement of the target. Jun 10 2016 - 4:14am
DESCRIPTION Quizartinib (AC220) is an inhibitor of class III receptor tyrosine kinases (FLT3, CSF1 receptor, KIT, PDGF receptors). It was developed to treat oncogenic FLT3 activation in acute myeloid leukemia. It is compound 7 in . (GtoPdb)
DESCRIPTION Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis[1].
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION inhibtor of VEGFR3 (Informer Set)
DESCRIPTION On July 2023, FDA approved Quizartinib to use as part of a treatment regimen for newly diagnosed acute myeloid leukemia that meets certain criteria (PKIDB)
DESCRIPTION Potent Cdk2 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases. (TargetMol Bioactive Compound Library)
DESCRIPTION AC 220 dihydrochloride is a potent and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3) used for the treatment of AML. (BOC Sciences Bioactive Compounds)
Cell lines
30
Organisms
0
Compound Sets
32
AdooQ Bioactive Compound Library
A10027
Axon Medchem Screening Library
1696
BOC Sciences Bioactive Compounds
ac-220-dihydrochloride-cas-1132827-21-4-item-160999
Cayman Chemical Bioactives
17986
ChEMBL Approved Drugs
CHEMBL576982
CHEMBL2105709
ChEMBL Drugs
CHEMBL576982
CHEMBL2105709
Chemical Probes.org
ac220
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12874
DrugBank Approved Drugs
DB12874
DrugCentral
5341
DrugCentral Approved Drugs
5341
DrugMAP
DM8Y4JS
EU-OPENSCREEN Bioactive Compound Library
EOS101202
EUbOPEN Chemogenomics Library
EUB0000050
Guide to Pharmacology
5658
High-quality chemical probes
PD003221
Informer Set
640011
Kinase Inhibitors (best-in-class)
LINCS compound set
10037-101
10037-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL576982
CHEMBL2105709
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL576982
CHEMBL2105709
MedChem Express Bioactive Compound Library
HY-13001
HY-14217
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
AC-220
TargetMol Bioactive Compound Library
T2066
Tocris Bioactive Compound Library
6788
Tool Compound Set
Welcome Trust Cancer Drugs
254
External IDs
51
Properties
(calculated by RDKit )
Molecular Weight
560.22
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
6
Aromatic Ring Count
5
cLogP
5.86
TPSA
106.16
Fraction CSP3
0.34
Chiral centers
0.0
Largest ring
6.0
QED
0.26
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
FLT3
Tyrosine-protein kinase receptor FLT3
CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET
Ligands for Target Protein for PROTAC
Apoptosis related,FLT3,Target Protein Ligand
CSF1R
KIT
FLT3 (ITD)
FLT3 (WT)
Compound status
clinical
Pathway
RTK signaling
Angiogenesis
Apoptosis
Autophagy
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Known off targets
KIT, PDGFRA, PDGFRB, RET, and CSF1R
Kinase group
TK
MOA
FLT
Inhibitor
FLT3 inhibitor
Orthogonal probe
G749
Target class
Protein kinase
Kinase
Recommended Cell Concentration
100 nM
Source data