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Chemical Structure| 1922098-69-8 Chemical Structure| 1922098-69-8

Structure of CCG-222740
CAS No.: 1922098-69-8

Chemical Structure| 1922098-69-8

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CCG-222740 is a Rho/MRTF pathway inhibitor. It decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin (α-SMA) expression. It also modulates inflammatory components of the pancreas in KC mice (LSL-KrasG12D/+; Pdx-1-Cre) stimulated with caerulein.

Synonyms: CCG-222740

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Product Details of CCG-222740

CAS No. :1922098-69-8
Formula : C23H19ClF2N2O3
M.W : 444.86
SMILES Code : O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CC(F)(F)C1)NC4=CC=C(Cl)C=C4
Synonyms :
CCG-222740
MDL No. :MFCD32215314
InChI Key :PMTPYUTZAJWGPE-UHFFFAOYSA-N
Pubchem ID :121317937

Safety of CCG-222740

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of CCG-222740

GPCR
cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK-293T cells 30 μM Used in affinity pulldown experiments to identify pirin as a potential target via mass spectrometry ACS Pharmacol Transl Sci. 2019 Apr 12;2(2):92-100.
cancer-associated fibroblasts (CAFs) 10 μM 72 h To evaluate the effect of CCG-222740 on CAFs cell viability and collagen production, results showed that CCG-222740 decreased CAFs cell viability and reduced the levels of collagens I, 2a, IV, and α-SMA. Sci Rep. 2019 May 8;9(1):7072
mouse pancreatic stellate cells (PSCs) 1 μM 6 days To evaluate the effect of CCG-222740 on stellate cell activation, results showed that CCG-222740 significantly reduced the levels of α-SMA and collagen 2A. Sci Rep. 2019 May 8;9(1):7072
M229R 10 μM 72 h To evaluate the effect of CCG-222740 on the sensitivity of M229R cells to Vemurafenib. Results showed that CCG-222740 had a minor effect on M229R cells. Oncogene. 2020 Feb;39(7):1466-1483.
M229P 10 μM 72 h To evaluate the effect of CCG-222740 on the sensitivity of M229P cells to Vemurafenib. Results showed that CCG-222740 had a minor effect on M229P cells. Oncogene. 2020 Feb;39(7):1466-1483.
UACC62R 10 μM 72 h To evaluate the effect of CCG-222740 on the sensitivity of UACC62R cells to Vemurafenib. Results showed that CCG-222740 significantly increased the sensitivity of UACC62R cells to Vemurafenib. Oncogene. 2020 Feb;39(7):1466-1483.
UACC62P 10 μM 72 h To evaluate the effect of CCG-222740 on the sensitivity of UACC62P cells to Vemurafenib. Results showed that CCG-222740 increased the sensitivity of UACC62P cells to Vemurafenib. Oncogene. 2020 Feb;39(7):1466-1483.
human conjunctival fibroblasts 1.25, 2.5, 5, 10 μM 24 h To evaluate the effect of nanocarrier CCG-222740 on ACTA2 gene expression and cytotoxicity in human conjunctival fibroblasts. Results showed that nanocarrier CCG-222740 significantly decreased ACTA2 gene expression at 2.5, 5, and 10 μM concentrations and had no significant effect on cell viability. J Nanobiotechnology. 2018 Nov 27;16(1):97

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KC mice (LSL-KrasG12D/+; Pdx-1-Cre) Oral gavage 100 mg/kg Once daily for 7 days To evaluate the effect of CCG-222740 on stellate cell activation and immune cell infiltration in KC mice, results showed that CCG-222740 significantly reduced α-SMA levels, decreased macrophage infiltration, and increased CD4 T cells and B cells. Sci Rep. 2019 May 8;9(1):7072
New Zealand white rabbits Glaucoma filtration surgery model Subconjunctival injection 68 μg in 100 μl Single administration, observed for 30 days To evaluate the anti-fibrotic effect and safety of nanocarrier CCG-222740 in a rabbit glaucoma filtration surgery model. Results showed that nanocarrier CCG-222740 significantly prolonged bleb survival, reduced conjunctival scarring, and had no local or systemic toxicity. J Nanobiotechnology. 2018 Nov 27;16(1):97

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.24mL

2.25mL

1.12mL

22.48mL

4.50mL

2.25mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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