UNC5293 |
| رقم الكتالوجGC62516 |
UNC5293 هو مثبط قوي وانتقائي لـ MERTK (Ki = 190 بيكومول). يعمل UNC5293 على تثبيط MERTK (IC50 = 0.9 نانومتر) وهو أكثر انتقائية من Axl و Tyro3 و Flt3. يظهر UNC5293 خصائص PK الممتازة في الفئران ويستخدم في أبحاث سرطان الدم النخاعي.
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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