拉罗替尼
CAS号 | 1223403-58-4 | 货号 | BCP16262 |
中文名 | 拉罗替尼 | ||
英文名 | Larotrectinib | ||
中文别名 | |||
英文别名 | ARRY-470;ARRY 470;ARRY470;LOXO-101; LOXO-101; LOXO101; | ||
分子式 | C21H22F2N6O2 | 分子量 | 428.44 |
生物活性 | Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons. | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
靶 点 | Trk Receptor |
结构式
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