标签归档：unesbulin

Unesbulin(Synonyms: PTC596)

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Unesbulin (Synonyms: PTC596) 纯度: 98.22%

Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 (BMI-1) 抑制剂。Unesbulin 在急性髓细胞白血病 (AML) 细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡。Unesbulin 具有抗白血病作用。

Unesbulin(Synonyms: PTC596)

Unesbulin Chemical Structure

CAS No. : 1610964-64-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3237 In-stock
1 mg ￥1200 In-stock
5 mg ￥3000 In-stock
10 mg ￥4600 In-stock
25 mg ￥6800 In-stock
50 mg ￥9950 In-stock
100 mg 询价

* Please select Quantity before adding items.

Unesbulin 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity[1][2].

IC50 & Target

BMI-1[1]
体外研究
(In Vitro)

Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis[1].
Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1].
Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1].
Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2].

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.

Apoptosis Analysis[1]

Cell Line: AML cell lines (MOLM-13, OCI-AML3, MOLM-14, MV4-11, U-937, HL-60)
Concentration: 20, 50, 100, 200 nM
Incubation Time: For 48 hours
Result: Induced apoptosis in a dose- and time-dependent manner with the average IC50 and ED50 values among six cell lines were 30.7 nM and 60.3 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: MOLM-13 and U-937 cells
Concentration: 200 nM
Incubation Time: For 10 hours
Result: Led to an accumulation of cells in G2/M phase, whereas the percentage of cells in G1 phase decreased.

Western Blot Analysis[1]

Cell Line: MOLM-13 cell
Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time: For 20 hours
Result: Significantly reduced protein levels of BMI-1 and its downstream target ubiquitinated histone H2A.
Increased cyclin B1 and securin levels.

体内研究
(In Vivo)

Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival[1].
Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells[1].
Unesbulin (10 or 12.5  mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells[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: NOD-SCID/IL2Rγ-KO (NSG) mice with MOLM-13 cells[1]
Dosage: 5 mg/kg
Administration: Oral gavage; every 3 days for 13 days
Result: Significantly prolonged mouse survival compared with the vehicle-treated mice in a dose-dependent manner.

Clinical Trial

分子量

420.34

Formula

C19H13F5N6
CAS 号

1610964-64-1
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 : 16.67 mg/mL (39.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3790 mL 11.8951 mL 23.7903 mL
5 mM 0.4758 mL 2.3790 mL 4.7581 mL
10 mM 0.2379 mL 1.1895 mL 2.3790 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: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.97 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 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% corn oil

    Solubility: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.97 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 16.7 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]. Nishida Y, et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 2017 Feb 17;7(2):e527.

    [2]. BMI1 inhibitor PTC596

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