Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC₅₀=0.07 nM) 和 TRK (对 TRKA/B/C 的 IC₅₀=0.83/0.05/0.1 nM) 抑制剂。Repotrectinib 有效抑制 WT ALK (IC₅₀=1.01 nM)。Repotrectinib 具有抗癌活性。

Repotrectinib (TPX-0005) is a potent ROS1 (IC 50 =0.07 nM) and TRK (IC 50 =0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC 50 =1.01 nM). Repotrectinib has anti-cancer activity.

Solid

IC50: 0.07 nM (ROS1), 0.83/0.05/0.1 nM (TRKA/B/C), 1.01 nM (ALK), 1.04 nM (JAK2), 1.66 nM (LYN), 5.3 nM (Src), 6.96 nM (FAK)

Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC50=1.04, 1.66, 5.3, and 6.96 nM, respectively).
Repotrectinib effectively overcomes this primary resistance (IC50=100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50=13 nM) and the SRC substrate paxillin (IC50=107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. has not independently confirmed the accuracy of these methods. They are for reference only.

Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016
[2]. Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127.

In Vitro: DMSO : 25 mg/mL (70.35 mM; Need ultrasonic)配制储备液