您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > FB23-2
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
FB23-2
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。
FB23-2图片
CAS NO:2243736-45-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
FB23-2 是一种有效、选择性的 mRNA N6- 甲基腺嘌呤脱甲基酶FTO抑制剂,IC50值为 2.6 μM。FB23-2 具有抗增殖作用。FB23-2 能用于急性髓系白血病 (AML) 的研究。
生物活性

FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylaseFTO, with anIC50of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML)[1].

IC50& Target

IC50: 2.6 μM (FTO)[1]

体外研究
(In Vitro)

FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human AML cell line cells and primary blast AML cells[1].
FB23 inhibits the proliferation of NB4 and MONOMAC6 cells, with IC50values of 0.8 μM and 1.5 μM[1].
FB23-2 (20 μM; 72 hours) displays anti-proliferation effect via upregulating global m6A levels[1].
FB23-2 (0.5-5 μM; 24-72 hours) significantly suppresses the proliferation of BM cells from these two models in a dose-dependent manner[1].
FB23-2 exhibits FTO-dependent anti-proliferation activity and promotes myeloid differentiation and apoptosis[1].
FB23-2 (1-20 μM; 72 hours) significantly increases the mRNA and protein levels of ASB2 and RARA in NB4 and MONOMAC6 cells[1].
FB23-2 induces apoptosis (1-20 μM; 48-72 hours) and cell cycle arrest (5-20 μM; 24 hours) at G1 stage in AML cells[1].

Cell Proliferation Assay[1]

Cell Line:MA9 cells, FLT3ITD/NPM1 cells (mouse BM cells)
Concentration:0.5 μM, 2 μM, 5 μM
Incubation Time:24 hours, 48 hours, 72 hours
Result:Suppressed the proliferation of BM cells.

RT-PCR[1]

Cell Line:NB4 cells, MONOMAC6 cells
Concentration:1 μM, 5 μM , 20 μM
Incubation Time:72 hours
Result:Significantly increased ASB2 and RARA mRNA levels.

Apoptosis Analysis[1]

Cell Line:NB4 cells, MONOMAC6 cells
Concentration:1 μM, 5 μM , 20 μM
Incubation Time:48 hours (NB4 cells),72 hours (MONOMAC6 cells)
Result:Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line:MONOMAC6 cells
Concentration:5 μM , 20 μM
Incubation Time:24 hours
Result:Induced cell cycle arrest at G1 stage.
体内研究
(In Vivo)

FB23-2 (2 mg/kg; i.p.; daily; for 10 days) substantially suppresses leukemia progression and prolongs survival[1].
FB23-2 exhibits elimination half-life (rat 6.7 h) and Cmax(rat 2421.3 ng/mL) following intraperitoneal injection (rat 3 mg/kg)[1].

Animal Model:NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice, xeno-transplanted with MONOMAC6 AML cells[1]
Dosage:2 mg/kg
Administration:Intraperitoneal injection, daily, for 10 days
Result:Delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival.
Animal Model:Sprague Dawley (SD) rats[1]
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:Intraperitoneal injection
Result:T1/2(6.7 hours), Cmax(2421.3 ng/mL).
分子量

392.24

性状

Solid

Formula

C18H15Cl2N3O3

CAS 号

2243736-45-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL(63.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5495 mL12.7473 mL25.4946 mL
5 mM0.5099 mL2.5495 mL5.0989 mL
10 mM0.2549 mL1.2747 mL2.5495 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 (protect from light)。-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: 50%PEG300   50% saline

    Solubility: 10 mg/mL (25.49 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.37 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.30 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。