SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities^[1][2][3].

SC99 (10 or 30 μM; for 72 hours) induces MM cell death^[1].
SC99 (10 μM; 24 hours) decreases the p-STAT3 level but has no effects on total STAT3 expression. SC99 (2.5, 5, 10, 20 μM; for 60 mins) inhibits JAK2 phosphorylation in a concentration-dependent manner but does not inhibit the phosphorylation levels of AKT, ERK, mTOR or c-Src at a concentration up to 20 μM^[1].
SC99 (1.25, 2.5, 5 μM; pre-treated for 10 min) inhibits collagen (2 μg/mL) and thrombin (0.02 U/mL) induced phosphorylation of STAT3 in a concentration-dependent manner^[2].
SC99 (pre-treated for 2 hours) inhibits IL-6 (50 ng/ml; for 20 min) induced STAT3 nuclear translocation in OPM2 cells^[3].

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.

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models^[1].
SC99 (5, 10, 15 mM, 15 μL; ICV) produces an effective inhibitory effect on the phosphorylation of JAK2 and STAT3 in middle cerebral artery occlusion and reperfusion (MCAO/R) model (adult male SD rats; 250-300 g). SC99 ameliorates neuronal apoptosis and degeneration, neurobehavioral deficits, inflammatory response and brain edema^[3].

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.

336.15

C₁₅H₈Cl₂FN₃O

882290-02-0

Room temperature in continental US; may vary elsewhere.

DMSO : 83.33 mg/mL (247.90 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 (6.19 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (6.19 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

• 2.

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

  Solubility: 2.08 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (6.19 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 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

• [1]. Zubin Zhang, et al. A novel small molecule agent displays potent anti-myeloma activity by inhibiting the JAK2-STAT3 signaling pathway. Oncotarget. 2016 Feb 23;7(8):9296-308.

  [2]. Zhuan Xu, et at. A novel STAT3 inhibitor negatively modulates platelet activation and aggregation. Acta Pharmacol Sin. 2017 May;38(5):651-659.

  [3]. Yiping Ding, et al. Effects of SC99 on cerebral ischemia-perfusion injury in rats: Selective modulation of microglia polarization to M2 phenotype via inhibiting JAK2-STAT3 pathway. Neurosci Res. 2019 May;142:58-68.