产品信息
抗原名称
TRK
商品描述
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
分子量
526.51
纯度
>98%
可溶性
Ethanol ：93 mg/mL (176.6 mM)
DMSO ：93 mg/mL (176.6 mM)
DMSO ：93 mg/mL (176.6 mM)
外观
Powder
In vitro(体外研究)
ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.
In vivo(体内研究)
Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier.
背景
别名
LOXO101,LOXO 101
分子式
C21H22F2N6O2·H2O4S
CAS号
1223405-08-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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