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Regorafenib monohydrate
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。
Regorafenib monohydrate图片
CAS NO:1019206-88-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
BAY 73-4506 monohydrate
产品介绍
Regorafenib (BAY 73-4506) monohydrate 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,抑制VEGFR1/2/3PDGFRβKitRETRaf-1IC50分别为 13/4.2/46,22,7,1.5 和 2.5 nM。Regorafenib monohydrate 显示出非常强的抗肿瘤和抗血管生成活性。
生物活性

Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptortyrosine kinaseinhibitor, withIC50values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM forVEGFR1/2/3,PDGFRβ,Kit,RETandRaf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity[1].

IC50& Target[1]

Raf-1

2.5 nM (IC50)

VEGFR2

4.2 nM (IC50)

VEGFR1

13 nM (IC50)

BRafV600E

19 nM (IC50)

PDGFRβ

22 nM (IC50)

Braf

28 nM (IC50)

VEGFR3

46 nM (IC50)

体外研究
(In Vitro)

Regorafenib monohydrate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells[1].
Regorafenib monohydrate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2[1].
Regorafenib monohydrate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[3].

Cell Proliferation Assay[1]

Cell Line:GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells
Concentration:10 μM and 5 nM
Incubation Time:96 h
Result:Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.

Western Blot Analysis[1]

Cell Line:NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells
Concentration:0, 10, 30, 100, 300, 1000, 3000 nM
Incubation Time:30 min
Result:Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.
体内研究
(In Vivo)

Regorafenib monohydrate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model[1].
Regorafenib monohydrate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model[1].

Animal Model:Rat GS9L glioblastoma xenograft[1]
Dosage:10 mg/kg
Administration:Orally, single dose or daily for 4 days
Result:Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
Animal Model:Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors[1]
Dosage:0, 3, 10, 30, 100 mg/kg
Administration:Orally, qd × 9
Result:Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.
Clinical Trial
分子量

500.83

性状

Solid

Formula

C21H17ClF4N4O4

CAS 号

1019206-88-2

中文名称

瑞格非尼水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(99.83 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9967 mL9.9834 mL19.9669 mL
5 mM0.3993 mL1.9967 mL3.9934 mL
10 mM0.1997 mL0.9983 mL1.9967 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。-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: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 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。

*以上所有助溶剂都可在本网站选购。