[CAS NO. 841290-81-1]  R406

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PRODUCTS SPECIFICATIONS [841290-81-1]

Store
Catalog
SLK-S2194
Brand
Selleck
CAS
841290-81-1

DESCRIPTION [841290-81-1]

Overview

MDL-
Molecular Weight628.63
Molecular FormulaC22H23FN6O5.C6H6O3S
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.5908 mL7.9538 mL15.9076 mL
5 mM0.3182 mL1.5908 mL3.1815 mL
10 mM0.1591 mL0.7954 mL1.5908 mL
50 mM0.0318 mL0.1591 mL0.3182 mL

Description

R406 is a potent inhibitor with of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces . Phase 1.

Features

Lead drug candidate for rheumatoid arthritis.

Targets

Flt3 [1]
(Cell-free assay)
Syk [1]
(Cell-free assay)
41 nM

In vitro

R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling. R406 inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 binds to the ATP binding pocket of Syk and inhibits its kinase activity as an ATP-competitive inhibitor with K of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes. R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurselike cells cocultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering. R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients.