XAV-939 是一种 Tankyrase 抑制剂。XAV-

XAV-939 

XAV-939 是一种 Tankyrase 抑制剂。XAV-939 对 TNKS1 和 TNKS2 具有抑制活性，IC₅₀ 值分别为 5 nM 和 2 nM。XAV-939 也是 hMSCs 成骨细胞分化的增强剂。XAV-939 可用于研究与激活的 Wnt 信号传导相关的疾病，例如癌症、纤维化疾病和与低骨形成相关的疾病。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性    
XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation

体外研究(In Vitro)    
XAV-939 has activity against TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively[1].
? XAV-939 (0.3-30 μM; 3 or 10 days) enhances osteoblast differentiation of hBMSCs[2].
? XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2[2].
? XAV-939 (3 μM; 10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation[2].
? XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression[3].

Cell Viability Assay[2]

Cell Line:    hMSC-TERT cell line
Concentration:    0.3, 3, and 30 μM
Incubation Time:    3 days
Result:    Showed no significant effect on proliferation at day 1, 2, and 3 at dose of 0.3 and 3 μM but inhibited hMSCs cell proliferation on day 3 at dose of 30 μM.

体内研究
(In Vivo)    
XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo[3].

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

分子量    
312.31

性状    
Solid

Formula    
C14H11F3N2OS

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 : 15.62 mg/mL (50.01 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    3.2019 mL    16.0097 mL    32.0195 mL
5 mM    0.6404 mL    3.2019 mL    6.4039 mL
10 mM    0.3202 mL    1.6010 mL    3.2019 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: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

2.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

3.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: 1.56 mg/mL (5.00 mM); Clear solution; Need ultrasonic
 

参考文献

[1]. Mohit Narwal, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9.  [Content Brief] [2]. Nuha Almasoud, et al. Tankyrase inhibitor XAV-939 enhances osteoblastogenesis and mineralization of human skeletal (mesenchymal) stem cells. Sci Rep. 2020 Oct 7;10(1):16746.  [Content Brief] [3]. Senxin Cai, et al. Mechanical stress reduces secreted frizzled-related protein expression and promotes temporomandibular joint osteoarthritis via Wnt/β-catenin signaling. Bone. 2022 Aug;161:116445.  [Content Brief]

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