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IQS-019 mesylate

Chemical Structure : IQS-019 mesylate

CAS No.: 1630804-27-1

IQS-019 mesylate (IQS 019;IQS019)

Catalog No.: PC-60404Not For Human Use, Lab Use Only.

A novel, potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A novel, potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively; inhibits at least 20% of the kinase activity at 0.1 uM) and an almost complete kinase inactivation at the 10 uM in a set of 17 TK/TKLs; impaires cell proliferation, reduces CXCL12-dependent cell migration, and induces caspase-dependent apoptosis; shows improved efficacy in vitro and in vivo compared to ibrutinib.

Physicochemical Properties

M.Wt 606.523
Formula C26H29Cl2N7O4S
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

4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one methanesulfonate

References

1. Balsas P, et al. J Hematol Oncol. 2017 Mar 31;10(1):80.

2. Puig de la Bellacasa R, et al. Eur J Med Chem. 2014 Oct 30;86:664-75.

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