General
Preferred name
TANDUTINIB
Synonyms
MLN-518, CT-53518, MLN-0518 ()
MLN-518 ()
MLN518 ()
CT53518 ()
NSC726292 ()
Tandutinib (MLN518) ()
CT 53518 ()
Tandutinib (hydrochloride) ()
MLN518 (hydrochloride) ()
CT53518 (hydrochloride) ()
CT 53518, NSC726292, MLN518 ()
CT-53518 ()
MLN-0518 ()
NSC-759851 ()
P&D ID
PD003630
CAS
387867-13-2
1227636-17-0
2438900-70-8
Tags
available
drug candidate
obsolete probe
Drug indication
Anaplastic mixed oligoastrocytoma
clear cell renal carcinoma
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS MLN518 is a novel quinazoline-based small molecule inhibitor of the FLT3, KIT, and platelet-derived growth-factor receptor (PDGFR) tyrosine kinases with that has been shown to have great efficacy in murine models of FLT3 ITD-positive leukemia. Experiments with mice demonstrate that at effective concentrations, MLN518 has mild toxicity toward normal hematopoiesis for FLT3 ITD-positive leukemia. MLN518 has also been shown to preferentially inhibit the growth of blast colonies from FLT3 ITD-positive as compared to ITD-negative patients with AML, without significantly affecting colony formation by normal human progenitor cells. ; ;
DESCRIPTION Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 ¦ÌM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 ¦ÌM and 0.20 ¦ÌM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML)[1][2]. Tandutinib has the ability to cross the blood-brain barrier[3].
PRICE 29
DESCRIPTION Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 ??M), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
DESCRIPTION Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 ¦ÌM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 ¦ÌM and 0.20 ¦ÌM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML)[1][2]. Tandutinib hydrochloride has the ability to cross the blood-brain barrier[3].
DESCRIPTION inhibitor of c-KIT and VEGFR3 (Informer Set)
DESCRIPTION Investigated for use/treatment in leukemia (myeloid). (PKIDB)
DESCRIPTION Tandutinib, also known as MLN 518, is a piperazinyl quinazoline receptor tyrosine kinase inhibitor with antineoplastic activity. Tandutinib inhibits the autophosphorylation of FLT3 (FMS-Like Tyrosine kinase-3), c-KIT and PDGF (platelet-derived growth factor) receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. (BOC Sciences Bioactive Compounds)
DESCRIPTION Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR. (TargetMol Bioactive Compound Library)
Cell lines
12
Organisms
1
Compound Sets
22
AdooQ Bioactive Compound Library
A10887
Axon Medchem Screening Library
1415
BOC Sciences Bioactive Compounds
tandutinib-cas-387867-13-2-343718
Cayman Chemical Bioactives
12098
ChEMBL Drugs
CHEMBL124660
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB05465
DrugMAP
DMNU2MH
Informer Set
464458
Ki Database
MLN-518
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL124660
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL124660
MedChem Express Bioactive Compound Library
HY-10202
HY-10202A
Novartis Chemogenetic Library (NIBR MoA Box)
Obsolete Compounds
tandutinib
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Tandutinib-(MLN518)
TargetMol Bioactive Compound Library
T1667
ZINC Tool Compounds
ZINC000003966243
External IDs
36
Properties
(calculated by RDKit )
Molecular Weight
562.33
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
1
Rotatable Bonds
10
Ring Count
5
Aromatic Ring Count
3
cLogP
5.03
TPSA
92.29
Fraction CSP3
0.52
Chiral centers
0.0
Largest ring
6.0
QED
0.34
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
FLT3
KIT
Apoptosis
c-Kit
CSF-1R
PDGFR
PDGFRβ
SRC
PDGFR¦Â
CSF1R, FLT3, KIT, PDGFD, PDGFRB
FLT3 inhibitor
PDGFD
Compound status
clinical
MOA
FLT antagonist
PDGFR inhibitor
Src antagonist
Flt3 (FLK2/STK1) Inhibitors
PDGFRbeta Inhibitors
KIT (C-KIT) Inhibitors
Angiogenesis Inhibitors
FLT3 inhibitor, KIT inhibitor, PDGFR tyrosine kinase receptor inhibitor
Member status
member
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Therapeutic Class
Anticancer Agents
Source data