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。
| 生物活性 | XAV-939 is aTankyraseinhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 withIC50values 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 activatedWntsignaling, such ascancer, fibrotic diseases and conditions associated with low bone formation[1][2][3]. |
| IC50& Target[6] | TNKS2 2 nM (IC50) | TNKS1 5 nM (IC50) | ARTD2 479 nM (IC50) | ARTD1 5500 nM (IC50) |
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体外研究
(In Vitro) | XAV-939 has activity against TNKS1 and TNKS2 with IC50values 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. |
Apoptosis Analysis[2] | Cell Line: | hMSC-TERT cell line | | Concentration: | 3 μM | | Incubation Time: | 3 days | | Result: | Showed a minute percentage of cell death (apoptosis and necrosis) in the XAV-939-treated hBMSC |
RT-PCR[2] | Cell Line: | hMSC-TERT cell line | | Concentration: | 3 μM | | Incubation Time: | 10 days | | Result: | Upregulated gene expression of osteoblast-associated gene markers including: ALP, COL1A1, RUNX2, and OC. |
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体内研究
(In Vivo) | XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo[3].
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 15.62 mg/mL(50.01 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 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℃, 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: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic
此方案可获得 1.56 mg/mL (5.00 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 15.6 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-CDin saline) Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic
此方案可获得 1.56 mg/mL (5.00 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 15.6 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。 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
此方案可获得 1.56 mg/mL (5.00 mM) 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 15.6 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。
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