Unesbulin PTC596|cas:1610964-64-1|西域试剂

Unesbulin PTC596,99.45%

产品编号：Bellancom-112041| CAS NO：1610964-64-1| 分子式：C₁₉H₁₃F₅N₆| 分子量：420.34

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货号	价格	库存与货期
Bellancom-112041	￥1200.00	杭州北京（现货）
Bellancom-112041	￥3000.00	杭州北京（现货）
Bellancom-112041	￥4600.00	杭州北京（现货）
Bellancom-112041	￥6800.00	杭州北京（现货）
Bellancom-112041	￥9950.00	杭州北京（现货）

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Unesbulin PTC596

产品介绍

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。

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.

体外研究

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.
Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase.
Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1.
Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1.

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

Apoptosis Analysis

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

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

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.
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.
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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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。