KJ Pyr 9 is an inhibitor ofMYCwith aK_dof 6.5 nM inin vitroassay.

Kd: 6.5±1.0 nM (MYC)^[1]

KJ Pyr 9 (KJ-Pyr-9) interferes with MYC-MAX complex formation in the cell, as shown in a protein fragment complementation assay. KJ Pyr 9 specifically inhibits MYC-induced oncogenic transformation in cell culture; it has no or only weak effects on the oncogenic activity of several unrelated oncoproteins. KJ Pyr 9 preferentially interferes with the proliferation of MYC-overexpressing human and avian cells and specifically reduces the MYC-driven transcriptional signature. KJ Pyr 9 against three cell lines is tested known to be dependent on increased MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT. The proliferation of all cell lines tested is inhibited, with IC₅₀values between 5 and 10 μM. Additionally, the proliferation of Burkitt lymphoma cell lines, which show constitutively high expression of c-MYC, is more sensitive to KJ Pyr 9 (IC₅₀values between 1 and 2.5 μM)^[1].

To test the in vivo effectiveness of KJ Pyr 9 (KJ-Pyr-9), nude mice receive a xenograft of MDA-MB-231 cells suspended in Matrigel and injected s.c. into the left and right flanks. When the tumors have reached an average volume of 100 mm³, mice are treated daily with 10 mg/kg KJ Pyr 9 or vehicle control by i.p. injection for 31 d. Inhibition of tumor growth by KJ Pyr 9 is noted after 8 d of treatment. By day 31, the tumor volume in the KJ Pyr 9-treated animals has not increased significantly. At the conclusion of the experiment the tumors are extracted and weighed. The weight measurements are in agreement with the volume determinations and confirmed the ability of KJ Pyr 9 to halt tumor growth^[1].

385.37

Solid

C₂₂H₁₅N₃O₄

581073-80-5

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL(324.36 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.49 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 900 μL20% 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
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.49 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。

• 3.

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

  Solubility: 2.08 mg/mL (5.40 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (5.40 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 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