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UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the research of acute leukemia. UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively. UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2.
| Molecular Weight | 476.66 |
| Formula | C28H40N6O |
| CAS Number | 1429881-91-3 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Zhang W,et.al. J Med Chem. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
| Related FLT3 Products |
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| KW-2449
KW-2449 is a novel multitargeted kinase inhibitor of FLT3, ABL and Aurora kinase with IC50 values of 6.6 nM, 14 nM and 48 nM. |
| Tandutinib
Tandutinib (MLN518, CT53518) is an orally active multitargeted tyrosine kinase inhibitor of FLT3 (IC50 = 0.22 μM), and it also inhibits c-Kit and PDGFR with IC50 values of 0.17 μM and 0.20 μM, respectively. Tandutinib has the ability to cross the blood-brain barrier. |
| TCS 359
TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. |
| CGP52421
CGP52421 is a FLT3 inhibitor, which is also an metabolite of midostaurin (PKC412). |
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