Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC₅₀ of 6 nM.

Mubritinib (TAK-165) specifically inhibits HER2 tyrosine kinase with an IC₅₀ 6 nM and does not inhibit other types tyrosine kinase up to 25 000 nM. Mubritinib inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). Mubritinib sensitivity depends on HER2 levels of each cell line. Especially, BT474 cells which over-express HER2 strongly is highly sensitive (IC₅₀=0.005 µM) and PC-3 cells which express HER2 very weakly is less sensitive (IC₅₀=4.62 µM). But, HT1376 and ACHN cells that over-expressed EGFR showed high IC₅₀ (IC₅₀>25 µM)^[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.

In the xenograft model, treatment with Mubritinib (TAK-165) significantly inhibits growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect after 14 days treatment are 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively^[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.

468.47

C₂₅H₂₃F₃N₄O₂

366017-09-6

木利替尼

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)

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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
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• 1.

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

  Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (5.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  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 (5.34 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.34 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]. Nagasawa J, et al. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92.

Cells are treated with Mubritinib at various concentrations (5 nM-25 μM) for 72 h. After the incubation period, the cells are counted. The IC₅₀ value is calculated from a dose-response curve generated by least-squares linear regression of the response^[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.

Mice: UMUC-3 and LN-REC4 cells are implanted with 50% Matrigel solution. After the tumor volume reaches 200–300 mm³ in LN-REC4 and UMUC-3 cells and to 100–200 mm³ in ACHN, the mice are treated orally twice daily for 14 days with vehicle (control) or 10 or 20 mg/kg per day of Mubritinib^[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.

• [1]. Nagasawa J, et al. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92.