2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. CCG-203971

CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent.

For research use only. We do not sell to patients.

CCG-203971 Chemical Structure

CCG-203971 Chemical Structure

CAS No. : 1443437-74-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 36 In-stock
Solution
10 mM * 1 mL in DMSO USD 36 In-stock
Solid
5 mg USD 33 In-stock
10 mg USD 60 In-stock
25 mg USD 120 In-stock
50 mg USD 180 In-stock
100 mg USD 288 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

CCG-203971 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent[1][2].

IC50 & Target

RhoA/MRTF-A[1]
In Vitro

CCG-203971, a second-generation Ras homolog gene family, member A (RhoA)/myocardin-related transcription factor A (MRTF-A)/serum response factor (SRF) pathway inhibitor, represses both matrix-stiffness and transforming growth factor beta–mediated fibrogenesis as determined by protein and gene expression in a dose-dependent manner. CCG-203971 significantly represses TGF-β- induced MKL1 expression at 25 μM concentration[2]. Human dermal fibroblasts are plated onto 96-well plates and allowed to grow for 3 days in the presence of 30 μM CCG-203971 or DMSO vehicle. Viable cell density is assessed through enzymatic reduction of the water-soluble tetrazolium dye WST-1. Scleroderma dermal fibroblasts proliferate faster than normal cells, and this is inhibited by CCG-203971[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CCG-203971 Related Antibodies
In Vivo

CCG-203971 is tested in a Bleomycin skin injury model. Bleomycin is administered in 50 μL of DMSO intraperitoneally. Preliminary studies show that Bleomycin administered in this manner is well tolerated at 100 mg/kg twice a day. Intradermal Bleomycin for 2 weeks along with the DMSO control (50 μL i.p.) results in marked dermal thickening (P<0.0001) compared with the PBS+DMSO group, which does not receive Bleomycin. CCG-203971 treatment strongly and significantly (P<0.001) suppresses the Bleomycin-induced skin thickening in this model. Skin collagen amounts, assessed by measurement of hydroxyproline content, show similar results. Bleomycin injections promote collagen deposition (P<0.01) and CCG-203971 is able to block this effect (P<0.05)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

408.88

Formula

C23H21ClN2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CCC1)NC4=CC=C(Cl)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (611.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4457 mL 12.2285 mL 24.4571 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.11 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (246 KB) HNMR (263 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[3]

Human dermal fibroblasts (2.0×104) are plated into a 96-well plate and grown overnight in DMEM containing 10% FBS. Media are removed and replaced with DMEM containing 2% FBS and 30 μM CCG-203971 or 0.1% DMSO control. After 72 hours WST-1 dye is added to each well, and after 60 minutes absorbance at 490 nm is read using a Wallac Victor2 plate reader[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Skin fibrosis is induced in C57BL/6 mice (female, 8 weeks old) by local intracutaneous injection of 100 μL of Bleomycin (1 mg/mL) in phosphate-buffered saline (PBS), every day for 2 weeks in a defined area (~1 cm2) on the upper back. Intracutaneous injection of 100 μL of PBS is used as a control. Three groups of mice with a total of 21 mice are used. One group receives injections of PBS and the other two are challenged with Bleomycin. Twice-a-day intraperitoneal administration of CCG-203971 (100 mg/kg in 50 μL of DMSO) is initiated together with the first challenge of Bleomycin and continues for 2 weeks. DMSO is used as the vehicle control. The three groups of animals are: (1) PBS/DMSO; (2) Bleomycin/DMSO; and (3) Bleomycin/CCG-203971. After treatment, animals are humanely killed by cervical dislocation, and tissue is collected[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4457 mL 12.2285 mL 24.4571 mL 61.1426 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL 12.2285 mL
10 mM 0.2446 mL 1.2229 mL 2.4457 mL 6.1143 mL
15 mM 0.1630 mL 0.8152 mL 1.6305 mL 4.0762 mL
20 mM 0.1223 mL 0.6114 mL 1.2229 mL 3.0571 mL
25 mM 0.0978 mL 0.4891 mL 0.9783 mL 2.4457 mL
30 mM 0.0815 mL 0.4076 mL 0.8152 mL 2.0381 mL
40 mM 0.0611 mL 0.3057 mL 0.6114 mL 1.5286 mL
50 mM 0.0489 mL 0.2446 mL 0.4891 mL 1.2229 mL
60 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0190 mL
80 mM 0.0306 mL 0.1529 mL 0.3057 mL 0.7643 mL
100 mM 0.0245 mL 0.1223 mL 0.2446 mL 0.6114 mL
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CCG-203971 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCG-2039711443437-74-8CCG203971CCG 203971RasRhoMKL1MRTFSRFPC-3migrationanti-metastasisInhibitorinhibitorinhibit

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