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Sorafenib Tosylate
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。
Sorafenib Tosylate图片
CAS NO:475207-59-1
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
500mg电议
1 g电议
5 g电议

产品名称
甲苯磺酸索拉非尼
Bay 43-9006 Tosylate
产品介绍
Sorafenib Tosylate (Bay 43-9006 Tosylate) 是一种有效的口服活性Raf抑制剂,对Raf-1B-RafIC50分别为 6 nM 和 20 nM。Sorafenib Tosylate 是一种多激酶抑制剂,对VEGFR2VEGFR3PDGFRβFLT3c-KitIC50分别为 90 nM,15 nM,20 nM,57 nM 和 58 nM。Sorafenib Tosylate 诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤活性。Sorafenib Tosylate 也是一种ferroptosis激动剂。
生物活性

Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally activeRafinhibitor withIC50s of 6 nM and 20 nM forRaf-1andB-Raf, respectively. SorafenibTosylate is a multikinase inhibitor withIC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM forVEGFR2,VEGFR3,PDGFRβ,FLT3andc-Kit, respectively. Sorafenib Tosylate inducesautophagyandapoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is aferroptosisactivator[1].

IC50& Target[1]

VEGFR3

20 nM (IC50)

Braf

22 nM (IC50)

Raf-1

6 nM (IC50)

VEGFR2

90 nM (IC50)

BrafV599E

38 nM (IC50)

PDGFRβ

57 nM (IC50)

c-Kit

68 nM (IC50)

Flt3

58 nM (IC50)

体外研究
(In Vitro)

Sorafenib Tosylate also inhibits BRAFwt(IC50=22 nM), BRAFV599E(IC50=38 nM), VEGFR-2 (IC50=90 nM), VEGFR-3 (IC50=20 nM), PDGFR-β (IC50=57 nM), c-KIT (IC50=68 nM), and Flt3 (IC50=58 nM) in biochemical assays[1]. Sorafenib-induced phosphorylation of c-Met, p70S6K and 4EBP1 is significantly reduced when 10-0505 cells are co-treated with anti-human anti-HGF antibody, suggesting that treatment with Sorafenib Tosylate leads to increased HGF secretion and activation of c-Met and mTOR targets[2].

体内研究
(In Vivo)

Sorafenib Tosylate (10, 30, 50 and 100 mg/kg, orally) treatment inhibits the tumor growth of 06-0606 and 10-0505 xenografts in a dose-dependent manner (P<0.01). The growth rate of 06-0606 and 10-0505 xenografts is also significantly reduced by Sorafenib. The weights of 06-0606 tumors in mice that are treated with Sorafenib 50 mg/kg and 100 mg/kg are approximately 13% and 5% of the controls, respectively. 50 mg dose of Sorafenib significantly inhibits tumor growth in mice with lines 5-1318, 26-1004 and 10-0505 (P<0.01). For 50 mg dose, the T/C ratio, where T and C are the median weight (mg) of Sorafenib- and vehicle-treated tumors at the end of the treatment, respectively, for 06-0606, 26-1004, 5-1318, and 10-0505 xenografts is 0.13, 0.10, 0.12 and 0.49, respectively[2]. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control[3].

Clinical Trial
分子量

637.03

性状

Solid

Formula

C28H24ClF3N4O6S

CAS 号

475207-59-1

中文名称

甲苯磺酸索拉非尼

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 : ≥ 31 mg/mL(48.66 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 mM1.5698 mL7.8489 mL15.6978 mL
5 mM0.3140 mL1.5698 mL3.1396 mL
10 mM0.1570 mL0.7849 mL1.5698 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。

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: 20%HP-β-CDin saline

    Solubility: 5 mg/mL (7.85 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: 2.08 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.27 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

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

    Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.27 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 20.8 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。