Repotrectinib(TPX-005)

产品编号: DC10463 Featured
Repotrectinib(TPX-005)
结构式
1802220-02-5
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中国地区超过5000个高品质化合物库存
应用领域
Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) 抑制剂. Repotrectinib (TPX-0005) 也有效抑制 WT ALK (1.01 nM) 和突变 ALKs,包括 ALK G1202R (1.26 nM),ALK L1196M (1.08 nM). Repotrectinib (TPX-0005) 也抑制其他多种酶,如 JAK2 (1.04 nM)、LYN (1.66 n
Cas No.: 1802220-02-5
名称: (13E,14E,3R,6S)-45-fluoro-3,6-dimethyl-5-oxa-2,8-diaza-1(5,3)-pyrazolo[1,5-a]pyrimidina-4(1,2)-benzenacyclononaphan-9-one
别名: TPX-0005,TPX 0005,TPX0005
SMILES: FC1=CC([C@@H](C)NC2=NC3=C4C=NN3C=C2)=C(O[C@@H](C)CNC4=O)C=C1
分子式: C18H18FN5O2
分子量: 355.37
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: TPX-0005, a novel ALK/ROS1/TRK inhibitor, effectively inhibited a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants. TPX-0005 is a small molecule kinase inhibitor — for the treatment of non–small cell lung adenocarcinoma with an ALK, ROS1, or NTRK mutation.TPX-0005 demonstrates potent inhibitory effects against solvent mutations after multiple treatments, including ALK G1202R, ROS1 G2032R, TRKA G595R, and TRKC G623R.The FDA based its approval on the findings from the ongoing TRIDENT-1 trial (ClinicalTrial.gov Identifier: NCT03093116), a “phase 1/2, open-label, multi-center, first-in-human study of the safety, tolerability, pharmacokinetics, and anti-tumor activity of TPX-0005 in patients with advanced solid tumors harboring ALK, ROS1, or NTRK1-3 rearrangements.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC10463 Repotrectinib(TPX-005) Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) 抑制剂. Repotrectinib (TPX-0005) 也有效抑制 WT ALK (1.01 nM) 和突变 ALKs,包括 ALK G1202R (1.26 nM),ALK L1196M (1.08 nM). Repotrectinib (TPX-0005) 也抑制其他多种酶,如 JAK2 (1.04 nM)、LYN (1.66 n