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CCG-222740

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Chemical Structure| 1922098-69-8 同义名 : -
CAS号 : 1922098-69-8
货号 : A1213276
分子式 : C23H19ClF2N2O3
纯度 : 99%+
分子量 : 444.858
MDL号 : MFCD32215314
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(269.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 In fibroblasts, the Rho/myocardin-related transcription factor (MRTF) pathway has classically been associated with cell contractility, and CAFs (Cancer associated fibroblasts) rely on this pathway to generate tracks for cancer cell migration. This pathway is implicated in the hyper-activation of fibroblasts in fibrotic diseases and the activation of pancreatic stellate cells. CCG-222740, a small molecule, is designed as a Rho/MRTF pathway inhibitor. PSCs (Pancreatic stellate cells), isolated as previously described from the pancreas of wild type C57BL/6 mice, were cultured for 3 days to achive confluence and then treated with CCG-222740 for 6 days. Treatment with 1 μM of CCG-222740 significantly (p < 0.05) reduced the levels of α-SMA (α smooth muscle actin; a marker for stellate cell activation) and collagen 2 A levels in the PSCs. CAFs isolated from a mouse pancreatic tumor induced by a Kras mutation were treated with several concentrations of CCG-222740 for 72 hours. This treatment decreased cell viability of CAFs, with an IC50 of ~10 μM, as measured by the MTT assay. CCG-222740 also had growth inhibitory effects on human and mouse pancreatic cancer cells, inducing growth arrest at similar concentrations as the CAFs. Moreover, CCG-222740 increased the protein levels of p27 and decreased cyclin D1, while the levels of collagens I, 2a and IV, as well as α-SMA in the CAFs were decreased after treatment with CCG-222740 for 72 hours. In vivo, CCG-222740 (100 mg/kg daily) by oral gavage significantly reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice (p < 0.05)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.24mL

2.25mL

1.12mL

22.48mL

4.50mL

2.25mL
参考文献

[1]Leal AS, Misek SA, Lisabeth EM, Neubig RR, Liby KT. The Rho/MRTF pathway inhibitor CCG-222740 reduces stellate cell activation and modulates immune cell populations in KrasG12D; Pdx1-Cre (KC) mice. Sci Rep. 2019;9(1):7072. Published 2019 May 8