QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC₅₀ of 35 nM^[1].

IC50: 35 nM (KDM4C)^[1]

QC6352 is a potent KDM4C inhibitor with an IC₅₀ of 35±8 nM^[1]. In a concentration-dependent manner QC6352 dramatically reduces the anchorage-independent sphere-forming capacity of BCSC1 and BCSC2. QC6352 blocks proliferation and self-renewal of BCSCs. As shown by western blot analysis the protein levels of (Epidermal growth factor receptor) EGFR are reduced in both BCSC1 and BCSC2 upon treatment with QC6352^[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.

QC6352 strongly affects tumor growth and final tumor weight of both BCSC1 and BCSC2 xenografts. Treatment with QC6352 is well tolerated and does not affect body weight of the mice. Results demonstrate that treatment with the KDM4 inhibitor QC6352 blocks BCSC xenograft tumor growth^[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.

387.47

C₂₄H₂₅N₃O₂

1851373-36-8

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 25 mg/mL (64.52 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： 50% PEG300    50% saline

  Solubility: 10 mg/mL (25.81 mM); Suspended solution; Need ultrasonic
• 2.

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

  Solubility: ≥ 1.67 mg/mL (4.31 mM); Clear solution

  此方案可获得 ≥ 1.67 mg/mL (4.31 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 16.7 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

• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 1.67 mg/mL (4.31 mM); Suspended solution; Need ultrasonic

  此方案可获得 1.67 mg/mL (4.31 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 4.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 1.67 mg/mL (4.31 mM); Clear solution

  此方案可获得 ≥ 1.67 mg/mL (4.31 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Chen YK, et al. Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models. ACS Med Chem Lett. 2017 Jul 27;8(8):869-874.

  [2]. Metzger E, et al. KDM4 inhibition targets breast cancer stem-like cells. Cancer Res. 2017 Sep 7. pii: canres.1754.

Cells are detached by Accutase and counted. 1×10³ single BCSC1 and BCSC2 cells are seeded as triplicates in 50% Matrigel into individual wells of 24-well ultra-low attachment plates in serum-free MSC medium. After 7 days, spheres over 50 μm diameter are counted for QC6352- and QC6688-treated and control cells and spheres over 20 μm diameter are counted for paclitaxel-treated and control cells^[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.

Mice: When tumors reach a palpable size of 3 mm³, mice are treated with vehicle (control) or QC6352. The inhibitor is administered daily to mice via oral gavage at 10 mg/kg. Control animals receive vehicle only. Animals are monitored twice weekly for weight and tumor growth^[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.

• [1]. Chen YK, et al. Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models. ACS Med Chem Lett. 2017 Jul 27;8(8):869-874.

  [2]. Metzger E, et al. KDM4 inhibition targets breast cancer stem-like cells. Cancer Res. 2017 Sep 7. pii: canres.1754.