UNC2025 |
| Catalog No.GC15556 |
UNC2025는 각각 0.74nM 및 0.8nM의 IC50 값을 갖는 강력하고 ATP 경쟁적이며 경구 활성이 높은 Mer/Flt3 억제제입니다. UNC2025는 Axl에 비해 MERTK에 대해 >45배 선택도입니다(IC50= 122 nM; Ki= 13.3 nM). UNC2025는 우수한 PK 특성을 나타내어 급성 백혈병 조사에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1429881-91-3
Sample solution is provided at 25 µL, 10mM.
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UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with the IC50 value of 0.8/0.74 nM for Mer/Flt3[1].
In vitro: In duplicate versus 305 kinases at Carna Biosciences using a microcapillary electrophoresis assay, UNC2025 inhibited Mer and Flt3 with the greatest potency. In B-ALL 697 cell lysates using the ATP ActivX probe assay, UNC2025 inhhibited the activity of Mer with an IC50 of 0.05 nM. In 697 B-ALL cells, UNC2025 potently inhibited Mer phosphorylation with an IC50 of 2.7 nM. Similarly, in Flt3-ITD positive Molm-14 acute myeloid leukemia cells, treatment with UNC2025 decreased phosphorylation of Flt3 with an IC50 of 14 nM. In soft agar cultures of the A549 NSCLC and Molm-14 AML cell lines, incubation withUNC2025 significantly inhibited colony formation, which was known to depend on Merand Flt3,respectively, for optimal expression of oncogenic phenotypes. Much higher concentrations of UNC2025 were required to effectively inhibit phosphorylation of Axl (IC50 = 122 nM) and Tyro3 (IC50 = 301 nM)[1].
In vivo: In mice with human leukemia xenografts, a single dose of UNC2025 (3 mg/kg) administered orally was sufficient to decrease Merphospho-protein levels in bone marrow leukemia cells by greater than 90% [1].
Reference:
[1]. Zhang W1,DeRyckere D,Hunter D,Liu J,Stashko MA,Minson KA, et,al. UNC2025, a potent and orally bioavailableMER/FLT3dual inhibitor.J Med Chem.2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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