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UNC2025

CAS No. : 1429881-91-3

MCE 站：UNC2025

产品活性：UNC2025 是一种强效、ATP 竞争性的，具有口服活性的 Mer/Flt3 抑制剂，IC₅₀ 值分别为 0.74 nM 和 0.8 nM。UNC2025 对MERTK 的选择性是 Axl 的 45 倍 (IC₅₀=122 nM; K_i=13.3 nM)。UNC2025 具有良好的 PK 特性，可用于急性白血病的研究。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FLT3

In Vitro: 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, 4.38nM, 5.75 nM, 5.83 nM, 6.14 nM,7.97 nM , 8.18 nM ａnd 364 nM, respectively.
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC₅₀ of 2.7 nM in 697 B-ALL cells.
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC₅₀ of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells.
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells.
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling ａnd colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells.
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.

In Vivo: UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), ａnd high oral exposure (100%), it shows T_max, C_max, ａnd AUClast 0.50 hour, 1.6 μM, ａnd 9.2 h μM, respectively.
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 ａnd 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 ａnd 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  CNS-Penetrant Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Sorafenib  |  Gilteritinib  |  Cabozantinib  |  Quizartinib  |  Crenolanib  |  Pacritinib  |  R406  |  Zotiraciclib  |  Fostamatinib  |  Ripretinib  |  Dovitinib  |  AT9283  |  Rebastinib  |  CA-4948  |  Sitravatinib  |  KW-2449  |  Gandotinib  |  Lestaurtinib  |  Linifanib  |  Merestinib  |  Amuvatinib  |  ENMD-2076  |  TG101209  |  FN-1501  |  MRX-2843  |  CHIR-124

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