Research Area
Product Type
United States ( Change Country )
Tandutinib (MLN518) Chemical Structure
Recommended Products
Cediranib (AZD2171)
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
Dovitinib (TKI-258)
Dovitinib(TKI-258) is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 5, 10, 8, 27, 36 nM for FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R, respectively.
Sunitinib Malate (Sutent)
Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 μM for Flk-1 and PDGFR
PHA-665752
PHA-665752 is c-Met inhibitor with an IC50 of 9 nM and Ki of 4 nM.
Vatalanib dihydrochloride (PTK787)
Vatalanib dihydrochloride (PTK787) is a novel VEGFR and c-Kit tyrosine kinases and angiogenesis inhibitor with IC50 of 0.037, 0.077, 0.27 and 0.73 μM for KDR, Flt-1, Flk and c-Kit, respectively.
XL-184 free base (Cabozantinib)
XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.
ENMD-2076
ENMD-2076 is a antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1.
MP-470 (Amuvatinib)
MP-470 (Amuvatinib) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM.
TSU-68 (SU6668)
TSU-68 (SU6668, Orantinib) is a potent inhibitor to receptor tyrosine kinases Flk-1/KDR, PDGFRβ, and FGFR1, with Ki of 2.1 μM, 1.2 μM, and 8 nM, respectively.
AEE788 (NVP-AEE788)
AEE788 (NVP-AEE788) is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelil growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1.
Biological Activity
The FMS-like tyrosine kinase 3 (FLT3) protein is a receptor tyrosine kinase that is expressed at high levels in 70-100% of cases of AML(Acute myeloid leukemia) and has been identified as potential target for molecular therapy. Internal tandem duplications (ITD) of the juxtamembrane domain in FLT3 occur regularly in de novo AML, resulting in constitutive activation of FLT3 tyrosine kinase activity. [1]
In cell-based assays tandutinib inhibited FLT3 ,PDGFR, and KIT with IC50 values of 95-122 ng/mL, but had no significant effect against a broad range of other kinases. In Ba/F3 cells expressing various FLT3-ITD mutants, tandutinib inhibited IL-3-independent growth and FLT3-ITD auto-phosphorylation with IC50 values of 6-17 ng/ml. Tandutinib also inhibited in vitro proliferation of human leukemia cell lines containing FLT3-ITD mutations with IC50 values of approximately 6 ng/mL. [2]
Tandutinib has a very limited spectrum of activity outside the type III receptor kinase family. Evaluation of tandutinib in rats, dogs, and monkeys showed it to be orally bioavailable, metabolically stable.
Phase I clinical results with tandutinib (MLN518) in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics.
References on Tandutinib (MLN518)
- [1] Cell Cycle 15 August 2009;8:16, 2621-263
- [2] Blood. 2006 December 1;108(12): 3674–3681.
Chemical Information
| Molecular Weight (WM): | 562.7 |
|---|---|
| Formula: | C31H42N6O4 |
| CAS No.: | 387867-13-2 |
| Synonyms: |
CT53518
|
| Dissolve in (25°C): | DMSO ≥11mg/mL |
| Water <1mg/mL | |
| Ethanol ≥19mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
Related Inhibitors
Recommended Screening Libraries
Chemical Library
A collection of 864 bioactive compounds
Inhibitor Library
A collection of 481 inhibitors
Kinase Inhibitor Library
A collection of 194 kinase inhibitors
Tyrosine Kinase Inhibitor Library
A collection of 85 tyrosine kinase inhibitors.
FDA Approved Drug Library
A collection of 426 FDA approved drugs
Natural Product Library
A collection of 139 natural products
Chemotherapeutic Agent Library
A collection of 40 chemotherapeutic agents
Epigenetics Compound library
A unique collection of 17 small molecule modulators
Stem Cell Compound library
A unique collection of 47 small molecule inhibitors
GPCR Compound library
A unique collection of 63 GPCR small molecules
Recently Viewed Items
Keywords:buy Tandutinib (MLN518) | Tandutinib (MLN518) supplier | purchase Tandutinib (MLN518) | Tandutinib (MLN518) cost | Tandutinib (MLN518) manufacturer | order Tandutinib (MLN518) | Tandutinib (MLN518) distributor