Takinib EDHS-206|cas:1111556-37-6|西域试剂

Takinib EDHS-206,99.31%

产品编号：Bellancom-103490| CAS NO：1111556-37-6| 分子式：C₁₈H₁₈N₄O₂| 分子量：322.36

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货号	价格	库存与货期
Bellancom-103490	￥1200.00	杭州北京（现货）
Bellancom-103490	￥1500.00	杭州北京（现货）
Bellancom-103490	￥6000.00	杭州北京（现货）
Bellancom-103490	￥11000.00	杭州北京（现货）

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Takinib EDHS-206

产品介绍

Takinib (EDHS-206) 是一种有效且选择性的 TAK1 抑制剂 (IC₅₀=9.5 nM)，比 IRAK4 (IC₅₀=120 nM) 和 IRAK1 (IC₅₀=390 nM) 作用强 1.5log 倍。Takinib 是一种TAK1自磷酸化的抑制剂，在 ATP 结合口袋内非竞争性结合。在类风湿关节炎和转移性乳腺癌细胞模型中，Takinib 诱导 TNF-α 刺激的细胞凋亡(apoptosis)。Takinib 也是恶性疟原虫蛋白激酶 9 (PfPK9) 的抑制剂 (K_D(app) of 0.46 nM)。

生物活性

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC₅₀=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (K_D(app) of 0.46 μM).

体外研究

Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells.
Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65.
Takinib serves as a chemical starting point for the development of PfPK9 (K_D(app) of 0.46 μM) inhibitors for malaria.
Takinib (2 hours; 0.1-20 µM; human RASFs) induces phosphorylation of TAK1^Thr184/187, STAT3^Tyr705 and STAT3^Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs^[4].

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

Western Blot Analysis

Cell Line:	Breast cancer cell line MDA-MB-231
Concentration:	10 μM
Incubation Time:	5, 15, 30, 60 minutes
Result:	IKK and p65 were maximally phosphorylated at 15 minutes, which indicated activation of the NF-κB pathway, while p38 phosphorylation peaks at 30 minutes.

Western Blot Analysis^[4]

Cell Line:	IL-1β-treated (10 ng/mL; 30 min) RASFs
Concentration:	0.1-20 µM
Incubation Time:	2 hours
Result:	Induced phosphorylation of TAK1^Thr184/187, STAT3^Tyr705 and STAT3^Ser727.

体内研究
(In Vivo)

Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis^[4].
Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice^[5].

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

Animal Model:	Male DBA/1 mice (CIA arthritis model)^[4]
Dosage:	50 mg/kg
Administration:	Intraperitoneally; daily from days 18-36
Result:	Showed a reduction in clinical arthritic score compared to vehicle control.

Animal Model:	Female NSG mice (8 weeks old)^[5]
Dosage:	50 mg/kg
Administration:	Oral gavage; daily until 17 days
Result:	Slowed tumor growth and reduced tumor size/weight.

体内研究

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

Animal Model:	Male DBA/1 mice (CIA arthritis model)^[4]
Dosage:	50 mg/kg
Administration:	Intraperitoneally; daily from days 18-36
Result:	Showed a reduction in clinical arthritic score compared to vehicle control.

Animal Model:	Female NSG mice (8 weeks old)^[5]
Dosage:	50 mg/kg
Administration:	Oral gavage; daily until 17 days
Result:	Slowed tumor growth and reduced tumor size/weight.

体内研究

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

Animal Model:	Male DBA/1 mice (CIA arthritis model)^[4]
Dosage:	50 mg/kg
Administration:	Intraperitoneally; daily from days 18-36
Result:	Showed a reduction in clinical arthritic score compared to vehicle control.

Animal Model:	Female NSG mice (8 weeks old)^[5]
Dosage:	50 mg/kg
Administration:	Oral gavage; daily until 17 days
Result:	Slowed tumor growth and reduced tumor size/weight.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (155.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1021 mL	15.5106 mL	31.0212 mL
5 mM	0.6204 mL	3.1021 mL	6.2042 mL
10 mM	0.3102 mL	1.5511 mL	3.1021 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: 2.5 mg/mL (7.76 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.76 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 25.0 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% corn oil
Solubility: 2.5 mg/mL (7.76 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.76 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。