CCG-1423

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CCG-1423

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:

285986-88-1

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
200mg	电议
500mg	电议
1 g	电议

产品介绍

CCG-1423 是Rho/MRTF/SRF通路的抑制剂。CCG-1423 在多种癌细胞中具有活性。CCG-1423 是开发新型药物工具的先导化合物，可用于癌症和糖尿病的研究。

生物活性

CCG-1423 is an inhibitor ofRho/MRTF/SRFpathway. CCG-1423 shows activities in severalcancercells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research ofcancerand diabetes^[1]^[2]^[3].

IC₅₀& Target

IC50: 1.5 μM (Rho-pathway selective serum response element-luciferase reporter)^[1]

体外研究
(In Vitro)

CCG-1423 (10 μM; 24 h) affects invasion by cultured PC-3 cells into a Matrigel matrix and inhibits 54% mitochondrial metabolism of WST-1^[1].
CCG-1423 (0-100 μM; 24 h) inhibits RhoA and RhoC signaling pathways with an IC₅₀value of 1.5 μM for Rho-pathway selective serum response element-luciferase reporter^[1].
CCG-1423 (1 μM; 16 h) improves glucose uptake in both L6 cells and primary human myotubes^[2].
CCG-1423 (10 μM; 18-19 h) inhibits expression of Rho downstream^[2].
CCG-1423 (3 μM; 25 h) selectively stimulates apoptosis of RhoC-overexpressing melanoma cell line (A375M2) compared with the parental cell line (A375)^[3].

Cell Invasion Assay^[1]

Cell Line:	PC-3 cell line
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Inhibited 71% invasion by cultured PC-3 cells into a Matrigel matrix.

Western Blot Analysis^[2]

Cell Line:	L6 myotubes
Concentration:	1 μM
Incubation Time:	48 hours
Result:	Increased insulin-stimulated Akt phosphorylation, blocked ERK phosphorylation, and increased IRS-1 tyrosine phosphorylation and its association with the p85 regulatory subunit of PI3K.

Cell Proliferation Assay^[3]

Cell Line:	PC-3 cell line
Concentration:	0.3 μM
Incubation Time:	8 days
Result:	Inhibited growth of PC-3 prostate cancer cells with an IC₅₀value of 1 μM with 30 μM LPA adding.

Apoptosis Analysis^[3]

Cell Line:	RhoC-overexpressing A375M2 and low RhoC-expressing A375 melanoma cell lines
Concentration:	3 μM
Incubation Time:	25 hours
Result:	Stimulated apoptosis of A375M2 cell line compared with the parental cell line.

体内研究
(In Vivo)

CCG-1423 (0.15 mg/kg; i.p. once daily for two weeks) affects glucose tolerance and insulin levels in HFD-fed mice^[1].

Animal Model:	16-week-old mice with HFD-induced obesity^[1]
Dosage:	0.15 mg/kg
Administration:	Intraperitoneal injection; 0.15 mg/kg once per day; for two weeks
Result:	Improved glucose tolerance and reduced insulin levels at 30 minutes after glucose injection.

分子量

454.75

性状

Solid

Formula

C₁₈H₁₃ClF₆N₂O₃

CAS 号

285986-88-1

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 : 100 mg/mL(219.90 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1990 mL	10.9951 mL	21.9901 mL
5 mM	0.4398 mL	2.1990 mL	4.3980 mL
10 mM	0.2199 mL	1.0995 mL	2.1990 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: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 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 25.0 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。