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SC-43
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。
SC-43图片
CAS NO:1400989-25-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
SC-43,Sorafenib 的衍生物,是一种有效的具有口服活性的SHP-1 (PTPN6)激动剂。SC-43 可抑制STAT3的磷酸化并诱导细胞凋亡 (apoptosis),具有抗纤维化和抗癌作用。
生物活性

SC-43, a Sorafenib derivative, is a potent and orally activeSHP-1 (PTPN6)agonist. SC-43 inhibits the phosphorylation ofSTAT3and induces cellapoptosis. SC-43 has anti-fibrotic and anticancer effects[1][2].

IC50& Target[1][2]

SHP-1

 

p-STAT3

 

体外研究
(In Vitro)

SC-43 (0-10 μM; 24-72 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment reveals the anti-proliferative effects in cholangiocarcinoma (CCA) cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively[1].
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines[1].
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level[1].
SC-43 activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. SC-43 augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition[1].

Cell Viability Assay[1]

Cell Line:HuCCT-1, KKU-100, and CGCCA cells
Concentration:0 μM, 0.25 μM, 0.5 μM, 0.75 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:24 hours, 48 hours, 72 hours
Result:Revealed the anti-proliferative effects in CCA cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively.

Cell Cycle Analysis[1]

Cell Line:HuCCT-1, KKU-100, and CGCCA cells
Concentration:0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:24 hours
Result:Showed increased sub-G1 cells and G2-M arrest.

Western Blot Analysis[1]

Cell Line:HuCCT-1, KKU-100, and CGCCA cells
Concentration:0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:24 hours
Result:Demonstrated significant increase in cleaved caspase-3 and PARP level.
体内研究
(In Vivo)

SC-43 (10-30 mg/kg; oral gavage; daily; for 23 days; male NCr athymic nude mice) treatment exhibits xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation[1].

Animal Model:Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells[1]
Dosage:10 mg/kg or 30 mg/kg
Administration:Oral gavage; daily; for 23 days
Result:Exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
Clinical Trial
分子量

431.80

性状

Solid

Formula

C21H13ClF3N3O2

CAS 号

1400989-25-4

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 : 250 mg/mL(578.97 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3159 mL11.5794 mL23.1589 mL
5 mM0.4632 mL2.3159 mL4.6318 mL
10 mM0.2316 mL1.1579 mL2.3159 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: 2.08 mg/mL (4.82 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.82 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
  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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。