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PROTAC-O4I2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC-O4I2图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

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 aPROTACtargets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with anIC50value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellularapoptosisin 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].

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 IC50of 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 IC50value of 63 nM).

Apoptosis Analysis[1]

Cell Line:K562 cell
Concentration:1 μM
Incubation Time:48 h
Result:Induced cellular apoptosis s in cells expressing SF3B1WTor SF3B1K700E.
体内研究
(In Vivo)

PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in aDrosophilaintestinal tumor model[1].

Animal Model:Drosophila melanogaster[1]
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.
分子量

609.10

性状

Solid

Formula

C29H29ClN6O5S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM1.6418 mL8.2088 mL16.4177 mL
5 mM0.3284 mL1.6418 mL3.2835 mL
10 mM0.1642 mL0.8209 mL1.6418 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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
*以上所有助溶剂都可在本网站选购。