XAV-939 - CAS:284028-89-3

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

规格

价格

是否有货

数量

5mg

In-stock

10mg

In-stock

25mg

In-stock

50mg

In-stock

100mg

In-stock

Other Forms of Rapamycin:

生物活性

XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC₅₀s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (K_ds of 99 and 93 nM, respectively).

体外研究

XAV939 also binds to recombinant PARP1, although with a significantly lower binding affinity (K_d=1.2 μM). XAV939 (1 μM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell. XAV939 (0.5 μM, 1.0 μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition. XAV-939 (10 nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells.

体内研究

XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model. XAV-939 (1 mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice.

分子式

C₁₄H₁₁F₃N₂Os

分子量

312.31

CAS号

284028-89-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (80.05 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

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 mg/mL (6.40 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (6.40 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 20.0 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。
2.请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: 2 mg/mL (6.40 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (6.40 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 20.0 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。
3.请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 1.04 mg/mL (3.33 mM); Clear solution

此方案可获得 ≥ 1.04 mg/mL (3.33 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 10.4 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

科研文献

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 69 篇科研文献

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