Sorafenib - CAS:284461-73-0

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

规格

价格

是否有货

数量

10mg

In-stock

50mg

In-stock

100mg

In-stock

500mg

In-stock

询价

In-stock

询价

In-stock

Other Forms of Rapamycin:

生物活性

Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC₅₀s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC₅₀s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.

IC₅₀&Target

VEGFR3

20 nM (IC₅₀)

Braf

22 nM (IC₅₀)

Raf-1

6 nM (IC₅₀)

VEGFR2

90 nM (IC₅₀)

PDGFRβ

57 nM (IC₅₀)

Braf

38 nM (IC₅₀)

c-Kit

68 nM (IC₅₀)

Flt3

58 nM (IC₅₀)

体外研究

Sorafenib (BAY 43-9006) also inhibits BRAF (IC₅₀=22 nM), BRAF (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. In MDA-MB-231 breast cancer cells, Sorafenib completely blocks activation of the MAPK pathway. Cells are preincubated with Sorafenib (0.01 to 3 μM), and dose-dependent inhibition of basal MEK 1/2 and ERK 1/2 phosphorylation (IC₅₀, 40 and 100 nM, respectively).

体内研究

Sorafenib demonstrates broad oral antitumor efficacy in panel of human tumor xenograft models. Sorafenib is given orally at 7.5 to 60 mg/kg. There is no lethality and no increase in weight loss in any treated group relative to the corresponding control group. Daily oral administration of Sorafenib (30 to 60 mg/kg) produces complete tumor stasis during treatment in five of the six models. 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.

分子式

C₂₁H₁₆ClF₃N₄O₃

分子量

464.83

CAS号

284461-73-0

中文名称

索拉非尼；索拉菲尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : ≥ 45 mg/mL (96.81 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1513 mL	10.7566 mL	21.5132 mL
5 mM	0.4303 mL	2.1513 mL	4.3026 mL
10 mM	0.2151 mL	1.0757 mL	2.1513 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: 2.08 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.47 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 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。