1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. TAS05567

TAS05567 

Cat. No.: HY-120214
Handling Instructions

TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.

For research use only. We do not sell to patients.

TAS05567 Chemical Structure

TAS05567 Chemical Structure

CAS No. : 1429038-15-2

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Description

TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases[1].

IC50 & Target

IC50: 0.37 nM (Syk); 10 nM (FLT3), 4.8 nM (JAK2), 600 nM (KDR) and 29 nM (RET)[1]

In Vitro

When Ramos cells (human B lymphoma cells) are pretreated with TAS05567 prior to BCR cross-linking by exposure to anti-IgM, there is marked inhibition of the phosphorylation of BLNK, an adaptor protein phosphorylated by activated Syk. The IC50 of TAS05567 for suppressing induction of BLNK phosphorylation by anti-IgM is 1.8 nM. TAS05567 also inhibits PLCγ2 (IC50 of 23 nM) and Erk1/2 (IC50 of 9.8 nM), after stimulation of Ramos cells with anti-IgM[1].
TAS05567 shows concentration-dependent inhibition of TNF-α production by THP-1 cells stimulated with IgG[1].
TAS05567 suppresses both calcium flux (IC50 of 27 nM) and histamine release (IC50 of 13 nM) induced by cross-linking of FcεRI with IgE and antigen[1].
TAS05567 inhibits the formation of mature osteoclasts in a concentration-dependent manner, and osteoclast differentiation is completely suppressed at 30 nM[1].

In Vivo

TAS05567 (10-30 mg/kg; oral administration; daily; for 9 days; female BALB/c mice) treatment suppresses hind-paw swelling in a dose-dependent manner. The serum MMP-3 levels are significantly lower in both the 10 mg/kg and 30 mg/kg TAS05567 groups than in the vehicle group[1].

Animal Model: Female BALB/c mice (7-8 weeks old) injected with collagen antibody[1]
Dosage: 10 mg/kg, 30 mg/kg
Administration: Oral administration; daily; for 9 days
Result: Suppressed hind-paw swelling in a dose-dependent manner.
Molecular Weight

439.51

Formula

C₂₁H₂₉N₉O₂

CAS No.

1429038-15-2

SMILES

O=C(C1=C(NC2=CC3=CN(C(C)(C)C)N=C3C(C)=C2)N=C(N[[email protected]]4[[email protected]@H](N)COCC4)N=N1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TAS05567TAS 05567TAS-05567SykSpleen tyrosine kinaseAutoimmuneanti-inflammatoryB-cellhistamineTNF-αFcγRcalciumfluxdifferentiationFLT3JAK2KDRRETInhibitorinhibitorinhibit

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TAS05567
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