| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CCG-1423 (CCG1423; CCG 1423) is a novel, potent and specific small-molecule inhibitor of RhoA signaling pathway with potential antitumor activity. It prevents transcription mediated by SRF. Several in vitro cancer cell functional assays show activity for CCG-1423. In PC-3 prostate cancer cells, CCG-1423 potently (<1 mumol/L) inhibits lysophosphatidic acid-induced DNA synthesis. At nanomolar concentrations, it also inhibits the growth of melanoma lines (A375M2 and SK-Mel-147) that overexpress RhoC, but it is less effective on related lines (A375 and SK-Mel-28) that express less Rho.
| Targets |
Rho-pathway selective serum response element-luciferase reporter (IC50 = 1.5 µM)
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
CCG-1423 is selective for Rho-overexpressing and invasive cancer cell lines, showing nanomolar to low micromolar potency in inhibiting DNA synthesis, cell growth, and/or invasion. Whereas the parental A375 cell line showed a smaller increase in Caspase-3 activation, daunorubicin showed the exact opposite pattern in the highly metastatic RhoC-overexpressing A375M2 melanoma cell line.
|
||
| Cell Assay |
In a 96-well plate coated with laminin, 2,000 cells in normal culture medium are plated per well. Following attachment, the medium is changed to serum-free medium (0% FBS) containing 30 μmol/L LPA, either in combination with or without 300 nM CCG-1423. To guarantee that LPA and compound are present for the duration of the experiment, fresh LPA, either with or without CCG-1423, is added on day 5. On day eight, the wells are filled with WST-1 reagent for one hour, and a Victor plate reader is used to measure the absorbance at 450 nm.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C18H13CLF6N2O3
|
|
|---|---|---|
| Molecular Weight |
454.75
|
|
| Exact Mass |
454.05
|
|
| Elemental Analysis |
C, 47.54; H, 2.88; Cl, 7.80; F, 25.07; N, 6.16; O, 10.55
|
|
| CAS # |
285986-88-1
|
|
| Related CAS # |
(S)-CCG-1423;2319939-24-5
|
|
| Appearance |
Solid powder
|
|
| SMILES |
CC(C(=O)NC1=CC=C(C=C1)Cl)ONC(=O)C2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F
|
|
| InChi Key |
DSMXVSGJIDFLKP-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C18H13ClF6N2O3/c1-9(15(28)26-14-4-2-13(19)3-5-14)30-27-16(29)10-6-11(17(20,21)22)8-12(7-10)18(23,24)25/h2-9H,1H3,(H,26,28)(H,27,29)
|
|
| Chemical Name |
N-[1-(4-chloroanilino)-1-oxopropan-2-yl]oxy-3,5-bis(trifluoromethyl)benzamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 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 25.0 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: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
 Forskolin-inhibits CCN1 expression via an MKL1 and SRF-dependent mechanism.J Mol Cell Cardiol. 2014 Nov 18;79C:157-168. |
|---|
 Binding of SRF to theSTARSpromoter.C. The SRF inhibitor CCG-1423 (1 µM) abolishedSTARS−365/+60 promoter-reporter activity in H9c2 cells (n = 3 experiments, in triplicates). PLoS One.2012;7(7):e40966. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA