CGI 1746

Pricing Availability   Qty
Description: Potent, reversible BTK inhibitor
Chemical Name: N-[3-[4,5-Dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)benzamide
Purity: ≥97%

Biological Activity for CGI 1746

CGI 1746 is a potent, reversible inhibitor of Bruton's tyrosine kinase (Btk) (IC50 = 1.9 nM). CGI 1746 decreases cell survival in prostate cancer cell lines. In a cell model, CGI 1746 blocks the production of FcγR-induced cytokines IL-1β, TNFα and IL-6 (IC50 values are 36 nM, 47 nM and 353 nM, respectively).

Technical Data for CGI 1746

M. Wt 579.7
Formula C34H37N5O4
Storage Store at -20°C
Purity ≥97%
CAS Number 910232-84-7
PubChem ID 24857323
Smiles CN1C=C(N=C(NC2=CC=C(C=C2)C(=O)N2CCOCC2)C1=O)C1=C(C)C(NC(=O)C2=CC=C(C=C2)C(C)(C)C)=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CGI 1746

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 11.59 20
DMSO 2.9 5

Preparing Stock Solutions for CGI 1746

The following data is based on the product molecular weight 579.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 8.63 mL 43.13 mL 86.25 mL
1 mM 1.73 mL 8.63 mL 17.25 mL
2 mM 0.86 mL 4.31 mL 8.63 mL
10 mM 0.17 mL 0.86 mL 1.73 mL

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References for CGI 1746

References are publications that support the biological activity of the product.

Di Paolo et al (2011) Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat.Chem.Biol. 7 41 PMID: 21113169

Kokabee et al (2015) Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol. Ther. 16 1604 PMID: 26383180

If you know of a relevant reference for CGI 1746, please let us know.

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Citations for CGI 1746

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