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UNC569

CAS No. : 1350547-65-7

MCE 站：UNC569

产品活性：UNC569 是一种有效、可逆、ATP 竞争性且具有口服活性的 Mer 激酶抑制剂，IC₅₀ 为 2.9 nM，K_i 为 4.3 nM。UNC569 还抑制 Axl 和 Tyro3，IC₅₀ 分别为 37 nM 和 48 nM。UNC569 可用于急性淋巴细胞白血病 (ALL) 和非典型畸胎瘤/横纹肌瘤的研究。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：TAM Receptor

In Vitro: UNC569 (24 hours) induces apoptosis in ALL cell lines, and increases the levels of cleaved Caspase 3 and cleaved PARP.
UNC569 (1 ?M; 1.5 hours) treatment effectively inhibit the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways.
UNC569 (1 hour) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, respectively.

In Vivo: The in vivo pharmacokinetic properties of UNC569 (3 mg/kg) are also assessed in mice via both intravenous (IV) and oral (PO) administration. UNC569 has low systemic clearance (19.5 mL/min/kg), high volume of distribution (V_ss of 5.83 L/kg), and good oral bioavailability (57%).
Leukemic zebrafish are treated continuously for 2 weeks by immersion in 4 ?M UNC569. the result shows that UNC569 induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  2-D08  |  SGI-7079  |  TAM-IN-2  |  RU-302

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