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CCG-222740

رقم الكتالوجGC38898

CCG-222740 هو مثبط مسار عامل النسخ المرتبط بـ Rho / myocardin النشط عن طريق الفم وانتقائي (MRTF)CCG-222740 هو أيضًا مثبط قوي لتعبير بروتين الأكتين للعضلات الملساء ألفايقلل CCG-222740 بشكل فعال من التليف في الجلد ويمنع ورم خبيث في الجلد

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CCG-222740 التركيب الكيميائي

Cas No.: 1922098-69-8

الحجم السعر المخزون الكميّة
5mg
279٫00
متوفر
10mg
441٫00
متوفر
25mg
783٫00
متوفر
50mg
1260٫00
متوفر
100mg
1710٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of CCG-222740

CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].

CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreased cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM[1]. CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts[2]. CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic[2]. Cell Cycle Analysis[1] Cell Line: Cancer associated fibroblasts (CAFs)

CCG-222740 (Oral gavage; 100 mg/kg daily for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice[1]. Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks[1]

[1]. Leal AS, et al. 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 May 8;9(1):7072. [2]. Yu-Wai-Man C, et al. Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis. Sci Rep. 2017 Mar 31;7(1):518.

Chemical Properties of CCG-222740

Cas No. 1922098-69-8 SDF
Canonical SMILES O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CC(F)(F)C1)NC4=CC=C(Cl)C=C4
Formula C23H19ClF2N2O3 M.Wt 444.86
الذوبان DMSO: 125 mg/mL (280.99 mM); Water: < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CCG-222740

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2479 mL 11.2395 mL 22.479 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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