UC-514321

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UC-514321  纯度: ≥98.0%

UC-514321 是NSC370284 的结构类似物，且活性更高，靶向STAT3/5 并选择性抑制TET1 的表达。UC-514321 体内体外均表现出良好的抗急性髓系白血病的活性，并具有较低的毒性。

UC-514321

UC-514321 Chemical Structure

CAS No. : 299420-83-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2810 In-stock
5 mg ￥2550 In-stock
10 mg ￥4550 In-stock
50 mg ￥13950 In-stock
100 mg   询价  
200 mg   询价  

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UC-514321 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
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生物活性

UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity[1].

IC50 & Target

STAT3

 

STAT5

 

体外研究
(In Vitro)

UC-514321 increases apoptosis in AML cells not in normal HSPCs[1].
UC-514321 (0-500 nM, 48 h) inhibits AML cells viability TET1-signaling dependently[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MONOMAC-6, THP-1, KOCL-48, KASUMI-1, ML-2, and NB4 cells.
Concentration: 0-500 nM.
Incubation Time: 48 hours.
Result: Most significantly repressed MONOMAC-6 cell viability.
Showed no inhibitory effect on the viability of TET1-low AML.

RT-PCR[1]

Cell Line: MONOMAC-6 cells.
Concentration: 0-500 nM.
Incubation Time: 48 hours.
Result: Functioned as TET1-transcription inhibitors in TET1-high AMLs and their anti-leukemic effects are TET1-dependent.

体内研究
(In Vivo)

UC-514321 (2.5 mg/kg, ip, once per day, for 10 days) exhibits more potent anti-tumor activity than NSC370284 in AML mice models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MLL-AF9-AML mice and AE9a-AML model[1].
Dosage: 2.5 mg/kg.
Administration: IP., once per day, for 10 days.
Result: Showed an improved therapeutic effect in AML mouse models in vivo.
Prolonged the median survival over three fold.

分子量

441.56

Formula

C26H35NO5
CAS 号

299420-83-0
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: 

Ethanol : 50 mg/mL (113.23 mM; Need ultrasonic)

DMSO : 25 mg/mL (56.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2647 mL 11.3235 mL 22.6470 mL
5 mM 0.4529 mL 2.2647 mL 4.5294 mL
10 mM 0.2265 mL 1.1323 mL 2.2647 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液。

    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 20% 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 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 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jiang X, et al. Targeted inhibition of STAT/TET1 axis as a therapeutic strategy for acute myeloid leukemia. Nat Commun. 2017 Dec 13;8(1):2099.

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