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CGI-1746

Chemical Structure : CGI-1746

CAS No.: 910232-84-7

CGI-1746 (CGI1746;CGI 1746)

Catalog No.: PC-42817Not For Human Use, Lab Use Only.

CGI-1746 is a potent, highly selective, second-generation BTK inhibitor with IC50 of 1.9 nM, displays 1,000-fold selectivity over Tec and Src family kinases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CGI-1746 is a potent, highly selective, second-generation BTK inhibitor with IC50 of 1.9 nM, displays 1,000-fold selectivity over Tec and Src family kinases.
CGI-1746 displays no significant binding affinity for other 385 kinases.
CGI-1746 abolishes FcγRIII-induced TNFα, IL-1β and IL-6 production in macrophages, blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis.
CGI-1746 inhibits myeloma-like tumors both in vitro and in vivo.

Physicochemical Properties

M.Wt 579.6887
Formula C34H37N5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)-

References

1. Di Paolo JA, et al. Nat Chem Biol. 2011 Jan;7(1):41-50.

2. Young WB, et al. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333-7.

3. Yang Y, et al. Cancer Res. 2015 Feb 1;75(3):594-604.

4. Kokabee L, et al. Cancer Biol Ther. 2015;16(11):1604-15.

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