Product Name :
TAS05567
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.
CAS:
1429038-15-2
Molecular Weight:
439.51
Formula:
C21H29N9O2
Chemical Name:
3-{[(3R,4R)-3-aminooxan-4-yl]amino}-5-[(2-tert-butyl-7-methyl-2H-indazol-5-yl)amino]-1,2,4-triazine-6-carboxamide
Smiles :
CC1=CC(=CC2=CN(N=C12)C(C)(C)C)NC1=NC(N[C@@H]2CCOC[C@@H]2N)=NN=C1C(N)=O
InChiKey:
ATERGQQFFHVNOJ-LSDHHAIUSA-N
InChi :
InChI=1S/C21H29N9O2/c1-11-7-13(8-12-9-30(21(2,3)4)29-16(11)12)24-19-17(18(23)31)27-28-20(26-19)25-15-5-6-32-10-14(15)22/h7-9,14-15H,5-6,10,22H2,1-4H3,(H2,23,31)(H2,24,25,26,28)/t14-,15+/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Oxacillin sodium salt} MedChemExpress|{Oxacillin sodium salt} Antibiotic|{Oxacillin sodium salt} Protocol|{Oxacillin sodium salt} In Vivo|{Oxacillin sodium salt} manufacturer|{Oxacillin sodium salt} Cancer}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.{{Moclobemide} site|{Moclobemide} Monoamine Oxidase|{Moclobemide} Protocol|{Moclobemide} In stock|{Moclobemide} custom synthesis|{Moclobemide} Cancer} 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.|Product information|CAS Number: 1429038-15-2|Molecular Weight: 439.51|Formula: C21H29N9O2|Chemical Name: 3-{[(3R,4R)-3-aminooxan-4-yl]amino}-5-[(2-tert-butyl-7-methyl-2H-indazol-5-yl)amino]-1,2,4-triazine-6-carboxamide|Smiles: CC1=CC(=CC2=CN(N=C12)C(C)(C)C)NC1=NC(N[C@@H]2CCOC[C@@H]2N)=NN=C1C(N)=O|InChiKey: ATERGQQFFHVNOJ-LSDHHAIUSA-N|InChi: InChI=1S/C21H29N9O2/c1-11-7-13(8-12-9-30(21(2,3)4)29-16(11)12)24-19-17(18(23)31)27-28-20(26-19)25-15-5-6-32-10-14(15)22/h7-9,14-15H,5-6,10,22H2,1-4H3,(H2,23,31)(H2,24,25,26,28)/t14-,15+/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.PMID:33070177 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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. TAS05567 shows concentration-dependent inhibition of TNF-α production by THP-1 cells stimulated with IgG. 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. TAS05567 inhibits the formation of mature osteoclasts in a concentration-dependent manner, and osteoclast differentiation is completely suppressed at 30 nM.|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.|Products are for research use only. Not for human use.|
