PROTAC-O4I2

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PROTAC-O4I2 

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)。

PROTAC-O4I2

PROTAC-O4I2 Chemical Structure

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5 mg ￥1600 询问价格 & 货期
10 mg ￥2500 询问价格 & 货期
25 mg ￥5500 询问价格 & 货期
50 mg ￥9500 询问价格 & 货期

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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[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells[1].
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[1].
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[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 Proliferation Assay[1]

Cell Line: K562 control cells (WT), cells overexpressing SF3B1 (OE), and cells expressing SF3B1K700E (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).

体内研究
(In Vivo)

PROTAC-O4I2 significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model[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.
分子量

609.10

Formula

C29H29ClN6O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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

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

*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]. Rodrigo A Gama-Brambila, et al. A PROTAC targets splicing factor 3B1. Cell Chem Biol. 2021 Nov 18;28(11):1616-1627.e8.

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