Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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CCG-222740 (CCG222740) is a novel and potent Rho/myocardin-related transcription factor (MRTF)/SRF inhibitor. CCG-222740 is also a potent inhibitor of the expression of the alpha-smooth muscle actin protein.
Targets |
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ln Vitro |
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ln Vivo |
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Cell Assay |
The culture medium used for murine cancer-associated fibroblasts (CAFs) contains 10% fetal bovine serum (FBS). After treating CAFs with various concentrations of CCG-222740 (740) for 72 hours, the levels of p27 and Cyclin D1 are assessed using western blotting.
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Animal Protocol |
Nine-week old KC mice
100 mg/kg Oral gavage |
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References |
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Molecular Formula |
C23H19CLF2N2O3
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Molecular Weight |
444.858371973038
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Exact Mass |
444.105
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Elemental Analysis |
C, 62.10; H, 4.31; Cl, 7.97; F, 8.54; N, 6.30; O, 10.79
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CAS # |
1922098-69-8
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Related CAS # |
1922098-69-8
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PubChem CID |
121317937
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Appearance |
Light yellow to yellow solid powder
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LogP |
4.4
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
4
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Heavy Atom Count |
31
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Complexity |
657
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Defined Atom Stereocenter Count |
0
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InChi Key |
PMTPYUTZAJWGPE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H19ClF2N2O3/c24-18-6-8-19(9-7-18)27-21(29)17-12-23(25,26)14-28(13-17)22(30)16-4-1-3-15(11-16)20-5-2-10-31-20/h1-11,17H,12-14H2,(H,27,29)
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Chemical Name |
N-(4-chlorophenyl)-5,5-difluoro-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide
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Synonyms |
CCG222740; CCG 222740; CCG-222740
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~125 mg/mL (~281 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.25 mg/mL (5.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2479 mL | 11.2395 mL | 22.4790 mL | |
5 mM | 0.4496 mL | 2.2479 mL | 4.4958 mL | |
10 mM | 0.2248 mL | 1.1239 mL | 2.2479 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Treatment with the Rho/MRTF pathway inhibitor CCG-222740 prevents the activation of primary stellate cells. Sci Rep . 2019 May 8;9(1):7072. td> |
Treatment with the Rho/MRTF pathway inhibitor CCG-222740 reduces viability and collagen production in cancer associated fibroblasts (CAFs) from Kras LSL-G12D; Trp53 LSL-R172H; Pdx1-Cre (KPC) mice. Sci Rep . 2019 May 8;9(1):7072. td> |
Rho/MRTF pathway inhibitor CCG-222740 decreases the levels α-SMA in KC mice stimulated with caerulein. Sci Rep . 2019 May 8;9(1):7072. td> |