UNC5293 |
| Katalog-Nr.GC62516 |
UNC5293 ist ein MERTK-selektiver und potenter Inhibitor (Ki=190 pM). UNC5293 hemmt MERTK (IC50=0,9 nM) und ist selektiver gegenüber Axl, Tyro3 und Flt3. UNC5293 zeigt ausgezeichnete PK-Eigenschaften bei Mäusen und wird für die Forschung zur Knochenmark-Leukämie eingesetzt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2226789-82-6
Sample solution is provided at 25 µL, 10mM.
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UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research[1].
UNC5293 provides selective target inhibition in cell-based assays. In cultures of the human B-cell acute lymphoblastic leukemia (B-ALL) cell line, UNC5293 inhibits phosphorylation of MERTK with an IC50 of 9.4 nM. In the SEM B-ALL cell line, UNC5293 is less potent against FLT3, with an IC50 of 170 nM[1].
UNC5293 (oral administration; 120 mg/kg; single dose) effectively inhibit MERTK in vivo in orthotopic 697 B-ALL mice xenografts[1].UNC5293 (oral gavage; 3 mg/kg; single dose) has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the Cmax and AUClast are 9.2 μM and 2.5 h*μM, respectively[1].
[1]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 May 17;220:113534.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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