Repotrectinib (TPX-0005) is a potent ROS1 (IC₅₀=0.07 nM) and TRK (IC₅₀=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC₅₀=1.01 nM). Repotrectinib has anti-cancer activity^[1][2].

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)^[1][2]

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)^[1].
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^[1].

上海金畔生物科技有限公司 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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

355.37

C₁₈H₁₈FN₅O₂

1802220-02-5

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 83.3 mg/mL (234.40 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.03 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.