SSTC3 是 casein 激酶1α(CK1α)的激动剂(Kd= 32 nM)，可抑制WNT信号 (EC50= 30 nM)。SSTC3 与其他类型的 WNT 抑制剂相比，具有极小的胃肠道毒性。
| 生物活性 | SSTC3 is acasein kinase1α (CK1α)activator (Kd= 32 nM) that inhibitsWNTsignaling (EC50= 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes ofWNTinhibitors[1]. |
体外研究
(In Vitro) | SSTC3 (0-1μM, 5 days) decreases the viability of HCT116 cells in an on-target manner. This capacity is significantly reduced when the mutant CTNNB1 allele driving its carcinogenic properties is deleted[1].
Cell Viability Assay[1] | Cell Line: | Colorectal cancer (CRC) cell lines. | | Concentration: | 0-1 μM. | | Incubation Time: | 5 days. | | Result: | Decreased the viability. |
Western Blot Analysis[1] | Cell Line: | SW403 cells. | | Concentration: | 100 nM. | | Incubation Time: | 15 min. | | Result: | Increased β-catenin phosphate levels. |
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体内研究
(In Vivo) | SSTC3 can be maintained for 24 hours after treatment[1].
SSTC3 (25 mg/kg, ip once daily for 8-12 days) suppresses the growth of colorectal carcinoma in CD-1 mice[1].
SSTC3 (10 mg/kg, ip once daily for 1 month) inhibits the growth of Apc mutation-driven tumors[1].
| Animal Model: | Five-week-old Apcminmice[1]. | | Dosage: | 10 mg/kg. | | Administration: | IP for 1 month. | | Result: | Inhibited the growth of Apc mutation-driven tumors. |
| Animal Model: | CD-1 mice. | | Dosage: | 25 mg/kg. | | Administration: | IP once daily for 8-12 days. | | Result: | Inhibited the growth of HCT116 xenografts.
Attenuated the growth of this metastatic CRC PDX and markedly reduced the cell density of residual cancer.
Reduced the expression of WNT biomarkers in this CRC PDX. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(241.07 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9285 mL | 9.6426 mL | 19.2853 mL | | 5 mM | 0.3857 mL | 1.9285 mL | 3.8571 mL | | 10 mM | 0.1929 mL | 0.9643 mL | 1.9285 mL |
*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。 In Vivo: 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 (4.01 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.01 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.01 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.01 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。 *以上所有助溶剂都可在本网站选购。
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