SC-43

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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。

CAS NO:

1400989-25-4

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

5 mg

10 mg

1 mM	2.3159 mL	11.5794 mL	23.1589 mL
5 mM	0.4632 mL	2.3159 mL	4.6318 mL
10 mM	0.2316 mL	1.1579 mL	2.3159 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。