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首页 / 抑制剂/激动剂 / 蛋白质酪氨酸激酶 / c-Kit / Dovitinib lactate

多韦替尼乳酸盐 /Dovitinib lactate {[allProObj[0].p_purity_real_show]}

货号：A445850 同义名： TKI-258 lactate;CHIR-258 lactate

Dovitinib lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

Dovitinib lactate 化学结构 CAS号：692737-80-7
Dovitinib lactate 化学结构
CAS号：692737-80-7
Dovitinib lactate 3D分子结构
CAS号：692737-80-7
Dovitinib lactate 化学结构 CAS号：692737-80-7
Dovitinib lactate 3D分子结构 CAS号：692737-80-7
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Dovitinib lactate 纯度/质量文件 产品仅供科研

货号：A445850 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		98%
Ki8751 ++

c-Kit, IC50: 40 nM

 		98+%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		98%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

 		Src 98%
Dasatinib ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dovitinib lactate 生物活性

描述 Fibroblast growth factors (FGFs) and FGF receptors (FGFRs) signaling network play essential roles to promote angiogenesis and tumor growth by binding to tyrosine kinase. Dovitinib (TKI258) is a small-molecule tyrosine kinase inhibitor targeting multiple RTKs, such as FGFRs. Dovitinib decreased the cell numbers in a dose-dependent manner in HCC1937 cells (IC50 = 13.8 μM), MCF-7 cells (IC50 = 12.7 μM), MDA-MB-231 cells (IC50 = 11.9 μM), MDA-MB-453 cells (IC50 = 9.7 μM), MDA-MB-468 cells (IC50 = 10.1 μM), and SK-BR-3 cells (IC50 = 11.7 μM). Dovitinib (0, 10, 15 μM; 24 h) induced the autophagy of various breast cancer cells through inhibiting STAT3/Mcl-1 axis in a dose-dependent manner. Treatment with 15 μM dovitinib induced about 15%, 40%, 25%, and 17% cell apoptosis at 24 h for MCF-7, MDA-MB-231, MDA-MB-468, and SK-BR-3 cells, respectively[3]. In mice bearing subcutaneous AN3CA, MFE296, SNGM, or HEC1A tumor xenografts, dovitinib (daily oral doses of 30 or 50 mg/kg) significantly delayed the growth of FGFR2-mutated endometrial cancer xenograft tumors. Of note, complete tumor regressions were observed in the majority of tumors at a dovitinib dose of 50 mg/kg in the SNGM xenograft model[4].

Dovitinib lactate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01678105 Recurrent Adenoid Cystic Carci... 展开 >>noma of the Salivary Glands Metastatic Adenoid Cystic Carcinoma of the Salivary Glands Salivary Gland Cancers ACC 收起 << Phase 2 Completed - Canada, Ontario ... 展开 >> Tom Baker Cancer Centre Calgary, Ontario, Canada, T2N 4N2 Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 London Health Sciences Centre London, Ontario, Canada, N6A 4L6 Ottawa Hospital Regional Cancer Centre Ottawa, Ontario, Canada, K1H 8L6 收起 <<
NCT01223027 Metastatic Renal Cell Carcinom... 展开 >>a 收起 << Phase 3 Completed - -
NCT01496534 Solid Tumors ... 展开 >>Bladder Cancer 收起 << Phase 1 Terminated(toxicity of combina... 展开 >>tion of medications) 收起 << - United States, New York ... 展开 >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 收起 <<

Dovitinib lactate 参考文献

[1]Huynh H, Chow PK, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012 Mar;56(3):595-601.

[2]Trudel S, Li ZH, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005 Apr 1;105(7):2941-8.

[3]Chiu YH, et al. Dovitinib Triggers Apoptosis and Autophagic Cell Death by Targeting SHP-1/p-STAT3 Signaling in Human Breast Cancers. J Oncol. 2019 Aug 14;2019:2024648.

[4]Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42.

Dovitinib lactate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.36mL

2.07mL

1.04mL

20.73mL

4.15mL

2.07mL

Dovitinib lactate 技术信息

CAS号692737-80-7
分子式C24H27FN6O4
分子量 482.507
别名 TKI-258 lactate;CHIR-258 lactate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 25 mg/mL(51.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Dovitinib | 692737-80-7 | CHIR-258 | TKI-258 | Tyrosine Kinase Inhibitor | Protein Tyrosine Kinase/RTK | FLT3 | c-Kit | FGFR | VEGFR | PDGFR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Dovitinib lactate 纯度/质量文件 | Dovitinib lactate 亚型比较 | Dovitinib lactate 生物活性 | Dovitinib lactate 临床数据 | Dovitinib lactate 参考文献 | Dovitinib lactate 实验方案 | Dovitinib lactate 技术信息

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