RK-287107|cas:2171386-10-8|西域试剂

RK-287107,99.81%

产品编号：Bellancom-123892| CAS NO：2171386-10-8| 分子式：C₂₂H₂₆F₂N₄O₂| 分子量：416.46

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货号	价格	库存与货期
Bellancom-123892	￥2500.00	杭州北京（现货）
Bellancom-123892	￥3800.00	杭州北京（现货）
Bellancom-123892	￥12000.00	杭州北京（现货）

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RK-287107

产品介绍

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 specific tankyrase inhibitor with IC₅₀s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.

体外研究

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.
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2.
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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 GI₅₀ value 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

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-week-old female NOD.CB17-Prkdc^scid/J mice with colorectal cancer COLO-320DM
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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-week-old female NOD.CB17-Prkdc^scid/J mice with colorectal cancer COLO-320DM
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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-week-old female NOD.CB17-Prkdc^scid/J mice with colorectal cancer COLO-320DM
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (300.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light)。-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。

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。
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 (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 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
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。