UNC1062 是一种MERTK选择性酪氨酸激酶抑制剂。UNC1062减少 MERTK 介导的下游信号传导的激活,在培养物中诱导细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis),减少软琼脂中的集落形成,并抑制黑色素瘤细胞的侵袭。UNC1062 能有效抑制 MERTK 激酶活性 (MERTK IC50=1.1 nM, Morrison Ki=0.33 nM),并在 TAM 家族中表现出特异性 (TYRO3 IC50=60 nM, AXL IC50=85 nM)。
产品描述
UNC1062 is a MERTK -selective tyrosine kinase inhibitor. UNC1062 reduces activation of MERTK-mediated downstream signaling, induces apoptosis in culture, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. UNC1062 potently inhibits MERTK kinase activity (MERTK IC 50 =1.1 nM, Morrison K i =0.33 nM) and exhibits specificity within the TAM family (TYRO3 IC 50 =60 nM, AXL IC 50 =85 nM) [1].
体外活性
UNC1062 potently inhibits MERTK kinase activity in vitro (MERTK IC50 = 1.1 nM, Morrison Ki = 0.33 nM) and exhibits specificity within the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). Treatment of HMCB and G361 cells with increasing concentrations of UNC1062 resulted in a potent dose-dependent reduction in MERTK phosphorylation[1].
Cas No.
1350549-36-8
分子式
C25H34N6O4S
分子量
514.64
别名
UNC 1025
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