Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity^[1][2].

Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI₅₀ 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT)^[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.

Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression^[2].
Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model^[2].
Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days)^[2].

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.

486.57

C₂₇H₃₀N₆O₃

1835667-12-3

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL (256.90 mM; Need ultrasonic)

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: ≥ 2.08 mg/mL (4.27 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.27 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.27 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763.

  [2]. Victoria L. Wilde, et al. Preclinical evidence of BPL-7711 activity in Egfr-mutant non-smallcell lung cancer ( NSCLC ) in orthotopically implanted human tumorxenografts in the lung and brain.