UNC 569 hydrochloride 是一种可逆的 ATP 竞争性 Mer 抑制剂,IC50 为 2.9 nM,Ki 为 4.3 nM。 UNC 569 hydrochloride 抑制 Axl 和 Tyro3,IC50 分别为 37 nM 和 48 nM。 UNC 569 hydrochloride 可用于关于急性淋巴细胞白血病和非典型畸胎样/横纹肌样肿瘤的研究。
产品描述
UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.
体外活性
UNC 569 hydrochloride inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL 697 and Jurkat cell lines, respectively. UNC 569 hydrochloride (1 μM) treatment effectively inhibits the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways. In ALL cell lines, UNC 569 hydrochloride (0.4 -2 μM) induces apoptosis and increases the levels of cleaved Caspase 3 and cleaved PARP[1].
体内活性
In Leukemic zebrafish, UNC 569 hydrochloride (4 μM) induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish[1]. UNC 569 hydrochloride has low systemic clearance (19.5 mL/min/kg), high volume of distribution (Vss of 5.83 L/kg), and good oral bioavailability (57%)[2].
Cas No.
T21302L
分子式
C22H30ClFN6
分子量
432.96
别名
UNC 569 hydrochloride (1350547-65-7 Free base)
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years