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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1429038-15-2
- 分子式: C21H29N9O2
- 分子量:439.51
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
化学情報
-
CAS 番号 1429038-15-2
-
分子量 439.51
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)