2. GPCR/G Protein MAPK/ERK Pathway Cytoskeleton Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt
  3. Ras ROCK
  4. CCG-222740

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

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CCG-222740 Chemical Structure

CCG-222740 Chemical Structure

CAS No. : 1922098-69-8

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10 mM * 1 mL in DMSO
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 USD 133 In-stock
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10 mM * 1 mL in DMSO USD 133 In-stock
Solid
5 mg USD 121 In-stock
10 mg USD 209 In-stock
25 mg USD 385 In-stock
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100 mg USD 1045 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CCG-222740 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Rho/MRTF pathway[1]
In Vitro

CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreases 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].

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

CCG-222740 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Cancer associated fibroblasts (CAFs)
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Increased the protein levels of p27 and decreased cyclin D1.
In Vivo

CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice[1].

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

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

444.86

Formula

C23H19ClF2N2O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CC(F)(F)C1)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 : 125 mg/mL (280.99 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 2.2479 mL 11.2395 mL 22.4790 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.25 mg/mL (5.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
  • Protocol 2

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

    Solubility: 2.25 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.25 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 (22.5 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.
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
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 2.2479 mL 11.2395 mL 22.4790 mL 56.1975 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL 11.2395 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 mL 5.6197 mL
15 mM 0.1499 mL 0.7493 mL 1.4986 mL 3.7465 mL
20 mM 0.1124 mL 0.5620 mL 1.1239 mL 2.8099 mL
25 mM 0.0899 mL 0.4496 mL 0.8992 mL 2.2479 mL
30 mM 0.0749 mL 0.3746 mL 0.7493 mL 1.8732 mL
40 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4049 mL
50 mM 0.0450 mL 0.2248 mL 0.4496 mL 1.1239 mL
60 mM 0.0375 mL 0.1873 mL 0.3746 mL 0.9366 mL
80 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
100 mM 0.0225 mL 0.1124 mL 0.2248 mL 0.5620 mL
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CCG-222740 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-2227401922098-69-8CCG222740CCG 222740RasROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKorallyRhomyocardin-relatedtranscriptionfactorMRTFalpha-smoothmuscleactinproteinexpressionfibrosismelanomametastasisInhibitorinhibitorinhibit

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