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Chemical Structure| 910232-84-7 Chemical Structure| 910232-84-7

Structure of CGI-1746
CAS No.: 910232-84-7

Chemical Structure| 910232-84-7

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CGI-1746 is a Bruton's tyrosine kinase (Btk) inhibitor.

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Product Details of CGI-1746

CAS No. :910232-84-7
Formula : C34H37N5O4
M.W : 579.69
SMILES Code : O=C(NC1=CC=CC(C(N=C2NC3=CC=C(C(N4CCOCC4)=O)C=C3)=CN(C)C2=O)=C1C)C5=CC=C(C(C)(C)C)C=C5
MDL No. :MFCD18782602
InChI Key :JIFCFQDXHMUPGP-UHFFFAOYSA-N
Pubchem ID :24857323

Safety of CGI-1746

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of CGI-1746

RTK

Isoform Comparison

Biological Activity

Target
  • BTK

    BTK, IC50:1.9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
human foreskin fibroblasts (HFFs) 5 μM 7 days Evaluate the effect of CGI-1746 on parasite plaque formation, showing a reduction in plaque area by approximately 91% Front Cell Infect Microbiol. 2023 Apr 3;13:1145824
OPM2 cells 0.2 μM to 50 μM 48 h Test the inhibitory effect of CGI1746 on HMCLs, showing IC50 of approximately 10 μM for ARP1 and OPM2 cells Cancer Res. 2015 Feb 1;75(3):594-604
ARP1 cells 0.2 μM to 50 μM 48 h Test the inhibitory effect of CGI1746 on HMCLs, showing IC50 of approximately 10 μM for ARP1 and OPM2 cells Cancer Res. 2015 Feb 1;75(3):594-604
MDA-MB-231 cells 20 μM 4 h RNA sequencing analysis of the effects of CGI-1746 on cells revealed that CGI-1746 alone significantly upregulated HSP70 gene expression iScience. 2024 Sep 24;27(11):110961
INA-6 cells 10 μM 48 h Evaluate the synergistic cytotoxic effect of CGI-1746 with the proteasome inhibitor LU-102, showing that CGI-1746 combined with LU-102 significantly reduced cell viability iScience. 2024 Sep 24;27(11):110961

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/KaLwRij mice 5TGM1 myeloma model Subcutaneous injection 100 mg/kg Three times per week, starting 7 days post-injection Test the therapeutic effect of CGI1746 on the 5TGM1 myeloma model, showing significantly prolonged median survival in the treatment group (57 days vs 39 days) Cancer Res. 2015 Feb 1;75(3):594-604

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.63mL

1.73mL

0.86mL

17.25mL

3.45mL

1.73mL

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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