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Regorafenib monohydrate

酪氨酸激酶抑制剂，Regorafenib monohydrate 是一种多靶点抑制剂，对VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1 的 IC50 分别为 13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM 和 2.5 nM。

目录号: PC16047 纯度: ≥98%

CAS No. :1019206-88-2

商品编号	规格	价格	会员价
PC16047-10mg	10mg	¥637.00	请登录
PC16047-50mg	50mg	¥1499.40	请登录
PC16047-100mg	100mg	¥1568.00	请登录
PC16047-200mg	200mg	¥2450.00	请登录
PC16047-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥686.00	请登录

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中文名称

Regorafenib monohydrate

中文别名

瑞格非尼(水合物);瑞格菲尼水合物;瑞格菲尼一水合物;瑞格菲尼一水物;瑞戈非尼一水合物;瑞格非尼一水合物;瑞戈非尼水合物;瑞格非尼;瑞格非尼-水合物;瑞格菲尼盐酸盐;（4R,5S）-4,5-二苯基-1,2,3-氧杂噻唑烷-2,2-二氧化物-3-羧酸叔丁基酯;4- [4 - [[[[4-氯-3-(三氟甲基)苯基]氨基]羰基]氨基] -3-氟苯氧基] -N-甲基-2-吡啶甲酰胺水合物;瑞格非尼水合物

英文名称

Regorafenib monohydrate

英文别名

4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate;Regorafenib monohydrate;Regorafenib hydrate;BAY 73-4506 Monohydrate;Regorafenib (BAY 73-4506)Monohydrate;Regorafenib monohydrate 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate;4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide,hydrate;4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate (1:1);Regorafenib (monohydrate);4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide;4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate;4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-pyridine-2-carboxylic acid methylamide monohydrate;MGN125FS9D;Regorafenib hydrate [JAN];Stivarga;Stivarga (TN);UNII-MGN125FS9D;Regorafenib monohydrate (BAY 73-4506);AK544054;Regorafenib hydrate (JAN);4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-n-methylpyridine-2-carboxamide;hydrate;4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}am

Cas No.

1019206-88-2

分子式

C₂₁H₁₇ClF₄N₄O₄

分子量

500.83

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

性状

Solid

IC50 & Target[1][2]

Raf-1

2.5 nM (IC₅₀)

VEGFR2

4.2 nM (IC₅₀)

VEGFR1

13 nM (IC₅₀)

BRaf

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.
Regorafenib monohydrate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.
Regorafenib monohydrate causes a concentration-dependent decrease in Hep3B cell growth, with an IC₅₀ of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.

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

Cell Proliferation Assay

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 IC₅₀ values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.

Western Blot Analysis

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 IC₅₀ values 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.
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.

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

Animal Model:	Rat GS9L glioblastoma xenograft
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
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255. [Information]

[2]. Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2(1), 39-49. [Information]

[3]. Carr BI, et al. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297. [Information]

溶解度数据

体外研究:

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9967 mL	9.9834 mL	19.9669 mL
5 mM	0.3993 mL	1.9967 mL	3.9934 mL
10 mM	0.1997 mL	0.9983 mL	1.9967 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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