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Takinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Takinib图片
CAS NO:1111556-37-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
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 1.5 log 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 (KD(app)of 0.46 nM)。
生物活性

Takinib (EDHS-206) is an orally active and selectiveTAK1inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets,IRAK4(120 nM) andIRAK1(390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib inducesapoptosisfollowing TNFα stimulation in cell models of rheumatoid arthritis and metastatic breastcancer. Takinib is also aP. falciparumprotein kinase 9(PfPK9)inhibitor (KD(app)of 0.46 μM)[1][2][3].

IC50& Target[1]

TAK1

9.5 nM (IC50)

IRAK4

120 nM (IC50)

IRAK1

390 nM (IC50)

GCK

430 nM (IC50)

CLK2

430 nM (IC50)

MINK1

1.9 μM (IC50)

体外研究
(In Vitro)

Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1].
Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65[1].
Takinib serves as a chemical starting point for the development ofPfPK9 (KD(app)of 0.46 μM) inhibitors for malaria[3].
Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705and STAT3Ser727in IL-1β-treated (10 ng/mL; 30 min) RASFs[4].

Western Blot Analysis[1]

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 TAK1Thr184/187, STAT3Tyr705and STAT3Ser727.
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].

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.
分子量

322.36

性状

Solid

Formula

C18H18N4O2

CAS 号

1111556-37-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM3.1021 mL15.5106 mL31.0212 mL
5 mM0.6204 mL3.1021 mL6.2042 mL
10 mM0.3102 mL1.5511 mL3.1021 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℃, 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: 2.5 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。

*以上所有助溶剂都可在本网站选购。