RK-287107 是一种有效的特异性tankyrase抑制剂，抑制tankyrase-1和tankyrase-2，IC50分别为 14.3 和 10.6 nM。RK-287107 可阻断结直肠癌细胞生长。
| 生物活性 | RK-287107 is a potent and specifictankyraseinhibitor withIC50s of 14.3 and 10.6 nM fortankyrase-1andtankyrase-2, respectively. RK-287107 blocks colorectalcancercell growth[1]. |
| IC50& Target[1] | tankyrase-1 14.3 nM (IC50) | tankyrase-2 10.6 nM (IC50) |
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体外研究
(In Vitro) | RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM[1].
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1].
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1].
Cell Proliferation Assay[1] | Cell Line: | Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells | | Concentration: | 0.01, 0.1, 1, 10 μM | | Incubation Time: | 12 hours | | Result: | Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1. |
Western Blot Analysis[1] | Cell Line: | COLO-320DM cells | | Concentration: | 0.03, 0.1, 0.33, 1, 3, and 10 μM | | Incubation Time: | 16 hours | | Result: | Downregulation of active β-catenin was observed |
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体内研究
(In Vivo) | RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model[1].
| Animal Model: | 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1] | | Dosage: | 100 and 300 mg/kg | | Administration: | Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks | | Result: | 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(300.15 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4012 mL | 12.0060 mL | 24.0119 mL | | 5 mM | 0.4802 mL | 2.4012 mL | 4.8024 mL | | 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 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 (protect from light)。-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 (4.99 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.99 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.99 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.99 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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