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CWI1-2

目录号 : GC68916

CWI1-2是一种选择性抑制m6A识别蛋白IGF2BP2的抑制剂,能够破坏IGF2BP2与m6A修饰的目标转录本之间的相互作用。

CWI1-2 Chemical Structure

Cas No.:2408590-36-1

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5mg
¥1,170.00
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10mg
¥1,980.00
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25mg
¥4,320.00
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50mg
¥7,020.00
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100mg
¥11,250.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

THP1

Preparation Method

Cells were treated with CWI1-2 (0.1-1 μM) for 48 h, cell viability was then evaluated by MTT assay. The medium was then changed with MTT solution (0.5mg/ml) in DMEM or RPMI without phenol red and FBS; cells were incubated at 37°C for 30 min and violet precipitate was dissolved with isopropanol. Absorbance at 550nm was measured through an EnSpire Multimode Plate reader.

Reaction Conditions

0.1 to1 μM, 48 hours

Applications

Treatment of THP1cells with CWI1-2 induced dramatic cell differentiation and apoptosis in a concentration-dependent manner

Animal experiment [2]:

Animal models

B6.SJL (CD45.1) mice

Preparation Method

B6.SJL (CD45.1) mice were performed bone marrow transplants (BMTs) using blast cells from MAP-induced leukemia mice or C1498 murine AML cells. Following the transplantation, CWI1-2 is administered at a dosage of 5 mg/kg daily via intravenous injection for a period of 7 to 10 days. Peripheral blood (PB) samples are then collected, and flow cytometric analysis is conducted to assess leukemia engraftment.

Dosage form

5 mg/kg/d, 7-10 days, i.v.

Applications

CWI1-2 treatment significantly delayed leukemia onset and prolonged the survival of BMT recipient mice

References:

[1]. Weng H, Huang F, Yu Z, et al. The m6A reader IGF2BP2 regulates glutamine metabolism and represents a therapeutic target in acute myeloid leukemia. Cancer Cell. 2022 Dec 12;40(12):1566-1582.e10. doi: 10.1016/j.ccell.2022.10.004.

产品描述

CWI1-2 is a selective inhibitor of the m6A reader protein IGF2BP2, disrupting the interaction between IGF2BP2 and m6A-modified target transcripts [1] [2]. The IC50 at the cellular level ranges from 203.1 to 781.6 nM[1] . This inhibitor is primarily used for research in acute myelocytic leukemia (AML) due to its promising anti-leukemic properties [1].

CWI1-2 exerts anti-leukemic effects by targeting IGF2BP2, inducing apoptosis and differentiation in leukemia cells. The IC50 at the cellular level ranges from 203.1 to 781.6 nM [1]. In AML cell lines, CWI1-2 at concentrations of 0.1 to1 μM over 48h inhibits cell growth and induces apoptosis [3].

CWI1-2 (5 mg/kg, intravenous injection, daily for 7-10 days) significantly reduced leukemia progression and prolonged survival in BMT recipient mice. Treatment results in a marked reduction in leukemia cell burden without significant changes in body weight [3].

References:
[1]. Zhu TY, Hong LL, Ling ZQ. Oncofetal protein IGF2BPs in human cancer: functions, mechanisms and therapeutic potential. Biomark Res. 2023 Jun 6;11(1):62. doi: 10.1186/s40364-023-00499-0.
[2]. Wang M, Chao M, Han H, et al. Hinokiflavone resists HFD-induced obesity by promoting apoptosis in an IGF2BP2-mediated Bim m6A modification dependent manner. J Biol Chem. 2024 Sep;300(9):107721. doi: 10.1016/j.jbc.2024.107721. Epub 2024 Aug 29. PMID: 39214307; PMCID: PMC11465056.
[3]. Weng H, Huang F, Yu Z, et al. The m6A reader IGF2BP2 regulates glutamine metabolism and represents a therapeutic target in acute myeloid leukemia. Cancer Cell. 2022 Dec 12;40(12):1566-1582.e10. doi: 10.1016/j.ccell.2022.10.004.

CWI1-2是一种选择性抑制m6A识别蛋白IGF2BP2的抑制剂,能够破坏IGF2BP2与m6A修饰的目标转录本之间的相互作用 [1][2]。该抑制剂在细胞水平的IC50范围为203.1至781.6 nM [1]。由于其显著的抗白血病特性,CWI1-2主要用于急性髓性白血病(AML)的研究[1]

CWI1-2通过靶向IGF2BP2发挥抗白血病作用,诱导白血病细胞的凋亡和分化。在细胞水平上的IC50范围为203.1至781.6 nM [1] 。在AML细胞系中,CWI1-2在0.1至1 μM浓度范围内作用48小时,可抑制细胞生长并诱导凋亡 [3]

CWI1-2(5 mg/kg,静脉注射,每日一次,连续7-10天)显著减缓了BMT受体小鼠白血病的进展,并延长了生存期。治疗结果显示,BMT受体小鼠白血病细胞负荷显著减少,且体重无明显变化 [3]

Chemical Properties

Cas No. 2408590-36-1 SDF Download SDF
分子式 C22H17Cl3N6O3 分子量 519.77
溶解度 DMSO : 100 mg/mL (192.39 mM; Need ultrasonic) 储存条件 Store at -20°C
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