UNC2025 HCI

UNC2025 HCI Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3. In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2] In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2]

• Einzelnachweise

  [1] Zhang W, et al. J Med Chem. 2014, 57(16), 7031-7041. [2] Cummings CT, et al. Mol Cancer Ther. 2015, 14(9), 2014-2022.

UNC2025 HCI Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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