1965323-05-0

Name	5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-, hydrochloride, hydrate (1:2:2)
CAS	1965323-05-0
Molecular Formula	C14H18ClF3N6O2
Molecular Weight	394.78
MOL File	1965323-05-0.mol

Synonyms

Syk Inhibitor II dihydrochloride dihydrate 5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-, hydrochloride, hydrate (1:2:2)

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Hazard Information

Uses

Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect[1].

in vivo

Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride dihydrate is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID₅₀ value of 13.2 mg/kg^[1].

IC 50

Syk: 41 nM (IC₅₀); serotonin: 460 nM (IC₅₀); PKCε: 5.1 μM (IC₅₀); PKCβ2: 11 μM (IC₅₀); ZAP-70: 11.2 μM (IC₅₀); Btk: 15.5 μM (IC₅₀); Itk: 22.6 μM (IC₅₀)

References

[1] Hiroyuki Hisamichi, et al. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure-activity relationships of pyrimidine-5-carboxamide derivatives. Bioorg Med Chem. 2005 Aug 15;13(16):4936-51. DOI:10.1016/j.bmc.2005.05.033

Supplier

Shandong Dayou Pharmaceutical Research and Development Co., Ltd.

Telephonehanfangpharma@126.com 15165037910

Websitehttps://hanfangpharma@126.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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