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TPCA-1
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。
TPCA-1图片
CAS NO:507475-17-4
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

产品介绍
TPCA-1 是一种有效,选择性的IKK-2抑制剂,IC50值为 17.9 nM。TPCA-1 也是STAT3磷酸化、DNA结合以及反式激活的有效抑制剂。
生物活性

TPCA-1 is a potent and selective inhibitor ofIKK-2withIC50of 17.9 nM. TPCA-1 is an effective inhibitor ofSTAT3phosphorylation, DNA binding, and transactivation.

IC50& Target[3]

IKK-2

17.9 nM (IC50)

STAT3

 

体外研究
(In Vitro)

TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50of 170 to 320 nM[1][2].
TPCA-1 (0-2 μM) inhibits STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner. TPCA-1 completely inhibits STAT3 phosphorylation without changing total STAT3 levels[3].
TPCA-1 increased sensitivity to ZD1839 in both TKI sensitive cells and insensitive cells[3].

Cell Viability Assay[2]

Cell Line:human peripheral blood monocytes stimulated with LPS.
Concentration:0-10 μM.
Incubation Time:~24 hours.
Result:TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes.

Cell Viability Assay[3]

Cell Line:HCC827 and H1975 cells.
Concentration:0-10 μM.
Incubation Time:0.5-2 hours.
Result:Suppressed proliferation of HCC827 and H1975 cells.
Led to a G2-M cell-cycle arrest in HCC827 but not A549.

Western Blot Analysis[3]

Cell Line:HEK-293T cell lines.
Concentration:0-2 μM (before IL-2 or IFN-α treatment).
Incubation Time:0.5-2 hours.
Result:Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.
体内研究
(In Vivo)

TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA)[2].
TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models[3].

Animal Model:10-12 weeks old male DBA/1 OlaHsd mice[2].
Dosage:3, 10, or 20 mg/kg.
Administration:I.P., b.i.d, from days 1 to 47.
Result:Reduced the severity and delays the onset of CIA.
Attenuated ex vivo antigen-induced T cell proliferation in CIA.
Animal Model:Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106)[3].
Dosage:10 mg/kg.
Administration:Intraperitoneally daily.
Result:The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(ETPCA-1), 0.680(EZD1839), and 0.837(Eobserved), respectively.
分子量

279.29

性状

Solid

Formula

C12H10FN3O2S

CAS 号

507475-17-4

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 : ≥ 100 mg/mL(358.05 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.5805 mL17.9025 mL35.8051 mL
5 mM0.7161 mL3.5805 mL7.1610 mL
10 mM0.3581 mL1.7903 mL3.5805 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: ≥ 7.5 mg/mL (26.85 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (26.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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% (20%SBE-β-CDin saline)

    Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (26.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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。

    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: ≥ 7.5 mg/mL (26.85 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (26.85 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 75.0 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。