TK216|cas:1903783-48-1|西域试剂

TK216,99.88%

产品编号：Bellancom-122903| CAS NO：1903783-48-1| 分子式：C₁₉H₁₅Cl₂NO₃| 分子量：376.23

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货号	价格	库存与货期
Bellancom-122903	￥1800.00	杭州北京（现货）
Bellancom-122903	￥3150.00	杭州北京（现货）
Bellancom-122903	￥6300.00	杭州北京（现货）
Bellancom-122903	￥11000.00	杭州北京（现货）

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TK216

产品介绍

TK216 是一种口服有效的 E26 转录因子 (ETS) 抑制剂。TK216 直接结合 EWS-FLI1 并抑制 EWS-FLI1 蛋白质相互作用。TK216 可以阻止 EWS-FLI1 与 RNA 解旋酶 A 的结合。TK216 具有抗癌活性。

生物活性

TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.

体外研究

TK216 (500 nM; for 24-72 hours) induces apoptosis in DLBCL cell lines.
TK216 (0.03, 0.06, 0.125, 0.25, 0.5 μM) results in a dose-dependent inhibition of proliferation in Ewing Sarcoma A4573 cell line.
TK216 (0.1, 0.3, 1 μM) induces apoptosis in DLBCL cell lines, with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control.
TK216 has IC₅₀s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line.
TK216 inhibits EWS-FLI1 (Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 fusion protein) protein interactions, leading to a decrease in transcription and proliferation.

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

Apoptosis Analysis

Cell Line:	DLBCL cell lines
Concentration:	500 nM
Incubation Time:	For 24, 48 or 72 hours
Result:	Induced apoptosis in DLBCL cell lines.

体内研究
(In Vivo)

TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model.

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

Animal Model:	NOD-Scid mice subcutaneously inoculated with TMD8 cells
Dosage:	100 mg/kg
Administration:	PO; twice daily for 13 days
Result:	Resulted in tumor growth inhibition.

体内研究

TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model.

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

Animal Model:	NOD-Scid mice subcutaneously inoculated with TMD8 cells
Dosage:	100 mg/kg
Administration:	PO; twice daily for 13 days
Result:	Resulted in tumor growth inhibition.

体内研究

TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model.

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

Animal Model:	NOD-Scid mice subcutaneously inoculated with TMD8 cells
Dosage:	100 mg/kg
Administration:	PO; twice daily for 13 days
Result:	Resulted in tumor growth inhibition.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 250 mg/mL (664.49 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6579 mL	13.2897 mL	26.5795 mL
5 mM	0.5316 mL	2.6579 mL	5.3159 mL
10 mM	0.2658 mL	1.3290 mL	2.6579 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。-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 (5.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.53 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 (5.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.53 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 (5.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.53 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。