PROTAC-O4I2|西域试剂

PROTAC-O4I2,98.96%

产品编号：Bellancom-141881| 分子式：C₂₉H₂₉ClN₆O₅S| 分子量：609.10

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货号	价格	库存与货期
Bellancom-141881	￥1600.00	杭州北京（现货）
Bellancom-141881	￥2500.00	杭州北京（现货）
Bellancom-141881	￥5500.00	杭州北京（现货）
Bellancom-141881	￥9500.00	杭州北京（现货）

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PROTAC-O4I2

产品介绍

PROTAC-O4I2 是一种靶向剪接因子 3B1 (SF3B1) 的 PROTAC。PROTAC-O4I2 在 K562 细胞中诱导 FLAG-SF3B1 降解，IC₅₀ 值为 0.244 μM。PROTAC-O4I2 还诱导 K562 WT 细胞凋亡 (apoptosis)。

生物活性

PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC₅₀ value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.

体外研究

PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells.
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 exhibits anti-proliferation effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC₅₀s of 228, 63, and 90 nM, respectively.
PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner with a half maximal inhibitory concentration (IC₅₀) value of 0.244 μM in K562 cells.

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

Cell Proliferation Assay

Cell Line:	K562 control cells (WT), cells overexpressing SF3B1 (OE), and cells expressing SF3B1^K700E (K700E)
Concentration:	1 pM, 0.1 nM, 10 nM, 1 μM, 100 μM
Incubation Time:	72 hours
Result:	In K562 WT cells, the parental compound O4I2 exhibited a marginal anti-proliferation effect (IC₅₀ >10 μM). In contrast, PROTAC-O4I2 showed significantly higher toxicity with an IC₅₀ of 228 nM, nearly 3-fold less potent than pladienolide B (IC₅₀, 76 nM). Cells overexpressing SF3B1 WT was slightly resistant to pladienolide B (IC₅₀, 134 nM), but more sensitive to PROTAC-O4I2 (an IC₅₀ value of 63 nM).

Apoptosis Analysis

Cell Line:	K562 cell
Concentration:	1 μM
Incubation Time:	48 h
Result:	Induced cellular apoptosis s in cells expressing SF3B1^WT or SF3B1^K700E.

体内研究
(In Vivo)

PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model.

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

Animal Model:	Drosophila melanogaster
Dosage:	10 μM
Administration:	Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days
Result:	Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.

体内研究

PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model.

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

Animal Model:	Drosophila melanogaster
Dosage:	10 μM
Administration:	Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days
Result:	Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.

体内研究

PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model.

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

Animal Model:	Drosophila melanogaster
Dosage:	10 μM
Administration:	Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days
Result:	Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (410.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6418 mL	8.2088 mL	16.4177 mL
5 mM	0.3284 mL	1.6418 mL	3.2835 mL
10 mM	0.1642 mL	0.8209 mL	1.6418 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: ≥ 2.08 mg/mL (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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