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Regorafenib monohydrate

现货
Catalog No.
A3751
酪氨酸激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 700.00
现货
10mg
¥ 650.00
现货
50mg
¥ 1,530.00
现货
100mg
¥ 1,600.00
Ship with 10-15 days
200mg
¥ 2,500.00
Ship with 10-15 days

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Background

Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RETand TIE2 [1].

Regorafenib is a multikinase inhibitor of both intracellular and membrane-bound RTKs. It shows potent inhibition of angiogenic and stromal RTKs like VEGF receptors-1-3, PDGFR-β and FGF receptor-1 with IC50 values ranging from4.2 to 311nM in biochemical assays. It also inhibits oncogenic RTKs, such as RET and c-KIT, with IC50 values ranging from 1.5 to 28nM in cellular assays [1].

Regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, GIST, and CRC with a mean IC50 value less than 1μM. These inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg [1].

References:
[1] Crona DJ, Keisler MD, Walko CM.Regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.Ann Pharmacother. 2013 Dec;47(12):1685-96.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt500.83
Cas No.1019206-88-2
FormulaC21H17ClF4N4O4
SynonymsBAY 73-4506 monohydrate
Solubility≥25.05 mg/mL in DMSO, <1.63 mg/mL in H2O
Chemical Name4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate
SDFDownload SDF
Canonical SMILESCNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F.O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人脐血管内皮和人主动脉平滑肌细胞

溶解方法

在DMSO中的溶解度>25.1mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

IC50: 2.6和146 nM

应用

Regorafenib有效地抑制了VEGF和FGF-2刺激的人脐血管内皮细胞和用PDGF的BB二聚糖蛋白刺激的人主动脉平滑肌细胞的增殖,IC50值分别为2.6和146 nM。

动物实验[1]:

动物模型

CRC、乳腺癌和肾细胞癌小鼠异种移植模型

剂量

10-100 mg/kg

应用

在CRC、乳腺癌和肾细胞癌小鼠异种移植模型中,Regorafenib monohydrate以剂量依赖的方式抑制肿瘤生长。Regorafenib也降低了pERK1/2,表明Regorafenib的抗增殖作用是通过RAF/MEK/ERK信号传导级联抑制。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Crona DJ, Keisler MD, Walko CM.Regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.Ann Pharmacother. 2013 Dec;47(12):1685-96.

质量控制

化学结构

Regorafenib monohydrate

相关生物数据

Regorafenib monohydrate

相关生物数据

Regorafenib monohydrate