1. Protein Tyrosine Kinase/RTK Apoptosis JAK/STAT Signaling Stem Cell/Wnt Epigenetics Neuronal Signaling
  2. Bcr-Abl Apoptosis STAT JAK Prion Protein
  3. Radotinib dihydrochloride

Radotinib dihydrochloride  (Synonyms: 雷多替尼二盐酸盐; IY-5511 dihydrochloride)

目录号: HY-179460
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Radotinib (IY-5511) dihydrochloride 是一种口服有效且能透过血脑屏障的选择性酪氨酸激酶 Bcr-Abl1 抑制剂,IC50 为 34 nM。Radotinib dihydrochloride 具有抗朊病毒和抗肿瘤的活性。Radotinib dihydrochloride 能够抑制肿瘤细胞增殖,诱导细胞周期阻滞和凋亡 (apoptosis)。Radotinib dihydrochloride 可用于慢性髓细胞白血病、多发性骨髓瘤等肿瘤和朊病毒病等神经退行性疾病的研究。

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Radotinib dihydrochloride

Radotinib dihydrochloride Chemical Structure

CAS No. : 926037-85-6

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Radotinib dihydrochloride 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

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生物活性

Radotinib (IY-5511) dihydrochloride is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib dihydrochloride has anti-prion and anti-tumor activities. Radotinib dihydrochloride can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib dihydrochloride can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases[1][2][3].

体外研究
(In Vitro)

Radotinib (0-100 μM; 72 h) dihydrochloride 能抑制多种多发性骨髓瘤细胞系的增殖,诱导细胞凋亡和细胞周期阻滞。机制涉及对 STAT3JAK2 信号通路的抑制[1]
Radotinib (0-40 μM; 24 h) dihydrochloride 在感染 22L 或 139A 瘙痒病株的 ZW13-2 神经元细胞中降低了 PrPSc水平[2]

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

Cell Viability Assay[1]

Cell Line: RPMI-8226, MM.1S, U266B1, and IM-9 cells
Concentration: 0, 10, 50 and 100 μM
Incubation Time: 72 h
Result: Inhibited the cell viability in a dose-dependent manner.
体内研究
(In Vivo)

Radotinib (100 mg/kg; 腹腔注射; 每天一次,除周末外; 21 天) dihydrochloride 在植入 IM-9 细胞的裸鼠模型中具有抗肿瘤的活性[1]
Radotinib (100 mg/kg; 灌胃; 4-8 周) dihydrochloride 在感染 263K 瘙痒病株的仓鼠中,可延长仓鼠的存活时间减少的 PrPSc 沉积[2]

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

Animal Model: Athymic nude male mice aged five weeks old treated IM-9 cells[1].
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; once a day except on weekends; 21 days
Result: Inhibited the growth of xenografted IM-9 cells in nude mice.
Repressed the expression of the activity and expression of STAT3, and its downstream proteins including Bcl-xL, Mcl-1, c-Myc, cyclin D1, and cyclin D3 in IM-9 cells isolated from the tumor tissue.
Dramatically reduced the expression of phospho-STAT3-positive cells in the tumor tissue.
Significantly increased the number of TUNEL-positive cells in the tumor tissue.
分子量

603.43

Formula

C27H23Cl2F3N8O

CAS 号
中文名称

雷多替尼二盐酸盐

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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Radotinib dihydrochloride
目录号:
HY-179460
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