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Regorafenib hydrochloride
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 hydrochloride图片
CAS NO:835621-07-3
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
瑞戈非尼盐酸盐
BAY 73-4506 hydrochloride
产品介绍
Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) 是一种多靶点抑制剂,靶作用于VEGFR1/2/3PDGFRβKitRETRaf-1IC50值分别为 13/4.2/46,22,7,1.5 和 2.5 nM。
生物活性

Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor forVEGFR1/2/3,PDGFRβ,Kit,RETandRaf-1withIC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[1].

IC50& Target[1]

VEGFR1

13 nM (IC50)

VEGFR2

4.2 nM (IC50)

VEGFR3

46 nM (IC50)

PDGFRβ

22 nM (IC50)

Braf

28 nM (IC50)

BRafV600E

19 nM (IC50)

Raf-1

2.5 nM (IC50)

体外研究
(In Vitro)

Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50of 3 nM[1]. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having 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].

体内研究
(In Vivo)

Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached[1].

Clinical Trial
分子量

519.28

性状

Solid

Formula

C21H16Cl2F4N4O3

CAS 号

835621-07-3

中文名称

瑞戈非尼盐酸盐;瑞格菲尼盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 5.6 mg/mL(10.78 mM)

H2O :< 0.1 mg/mL(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9257 mL9.6287 mL19.2574 mL
5 mM0.3851 mL1.9257 mL3.8515 mL
10 mM0.1926 mL0.9629 mL1.9257 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 (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。