TAS05567
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.
- CAS No.: 1429038-15-2
- Formula: C21H29N9O2
- Molecular Weight:439.51
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
IC50: 0.37 nM (Syk); 10 nM (FLT3), 4.8 nM (JAK2), 600 nM (KDR) and 29 nM (RET)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
Chemical Information
-
CAS No. 1429038-15-2
-
Molecular Weight 439.51
-
Formula C21H29N9O2
-
SMILES
O=C(C1=C(NC2=CC3=CN(C(C)(C)C)N=C3C(C)=C2)N=C(N[C@H]4[C@@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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz