Syk Inhibitor II dihydrochloride

Modify Date: 2024-01-14 13:09:57

Syk Inhibitor II dihydrochloride Structure
Syk Inhibitor II dihydrochloride structure
Common Name Syk Inhibitor II dihydrochloride
CAS Number 227449-73-2 Molecular Weight 449.25600
Density N/A Boiling Point N/A
Molecular Formula C14H21Cl2F3N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Syk Inhibitor II dihydrochloride


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

 Names

Name 2-(2-aminoethylamino)-4-[3-(trifluoromethyl)anilino]pyrimidine-5-carboxamide,dihydrate,dihydrochloride
Synonym More Synonyms

 Syk Inhibitor II dihydrochloride Biological Activity

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

5-HT Receptor:460 nM (IC50)

In Vitro Syk Inhibitor II (compound 9a) dihydrochloride 对 PKCε、PKCβ2、ZAP-70、Btk 和 Itk 的作用较弱,IC50 值分别为 5.1 µM、11 µM、11.2 µM、15.5 µM 和 22.6 µM[1]。
In Vivo Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride 在抗原攻击前 30 分钟皮下给药,以剂量依赖方式抑制过敏反应,ID50 值为13.2 mg/kg[1]。 Animal Model: ICR mice[1] Dosage: 10, 30, 100 mg/kg Administration: S.c.; 30 min before antigen challenge Result: Inhibited the anaphylaxis reaction dose-dependently with an ID50 value of 13.2 mg/kg.
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.  

 Chemical & Physical Properties

Molecular Formula C14H21Cl2F3N6O3
Molecular Weight 449.25600
Exact Mass 448.10000
PSA 144.86000
LogP 3.61220

 Synonyms

Syk Inhibitor II