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CGI1746

Item № 18414
CAS № 910232-84-7
Purity ≥98%
product image
                (CAS 910232-84-7)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $45.00 0.00
     5 mg $203.00 0.00
     10 mg $360.00 0.00
     25 mg $619.00 0.00

Pricing updated 2019-04-24. Prices are subject to change without notice.

Description

CGI1746 is a potent, selective inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 1.9 nM), a non-receptor tyrosine kinase that is important in B lymphocyte development.1,2 It blocks both auto-and trans-phosphorylation of BTK by occupying an SH3 binding pocket in the un-phosphorylated enzyme. CGI1746 prevents B-cell antigen receptor-mediated B lymphocyte proliferation and suppresses FCγRIII-induced TNFα, IL-1β, and IL-6 production in macrophages.1 It reduces cytokine levels within joints and ameliorates symptoms in a mouse model of autoantibody-induced arthritis.1

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Technical Information
Formal 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
CAS Number
910232-84-7
Molecular Formula
C34H37N5O4
Formula Weight
579.7
Purity
≥98%
Formulation
A crystalline solid
λmax
234, 355 nm
SMILES
O=C(C1=CC=C(NC2=NC(C3=CC=CC(NC(C4=CC=C(C(C)(C)C)C=C4)=O)=C3C)=CN(C)C2=O)C=C1)N5CCOCC5
InChI Code
InChI=1S/C34H37N5O4/c1-22-27(7-6-8-28(22)37-31(40)23-9-13-25(14-10-23)34(2,3)4)29-21-38(5)33(42)30(36-29)35-26-15-11-24(12-16-26)32(41)39-17-19-43-20-18-39/h6-16,21H,17-20H2,1-5H3,(H,35,36)(H,37,40)
InChI Key
JIFCFQDXHMUPGP-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. di Paolo, J.A., Huang, T., Balazs, M., et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis Nat.Chem.Biol. 7(1), 41-50 (2011).

2. Akinleye, A., Chen, Y., Mukhi, N., et al. Ibrutinib and novel BTK inhibitors in clinical development J. Hematol. Oncol. 6(59), (2013).

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