Product Name :
BAY-826
Description:
BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.
CAS:
1448316-08-2
Molecular Weight:
558.53
Formula:
C26H19F5N6OS
Chemical Name:
3-cyano-N-{2,4-dimethyl-5-[6-(pyridin-3-yl)-1H-pyrazolo[1,5-a]imidazol-1-yl]phenyl}-5-(pentafluoro-λ⁶-sulfanyl)benzamide
Smiles :
CC1C=C(C)C(=CC=1NC(=O)C1C=C(C=C(C=1)S(F)(F)(F)(F)F)C#N)N1C=CN2N=C(C=C21)C1=CN=CC=C1
InChiKey:
MPASHPJAIUOWCK-UHFFFAOYSA-N
InChi :
InChI=1S/C26H19F5N6OS/c1-16-8-17(2)24(36-6-7-37-25(36)13-23(35-37)19-4-3-5-33-15-19)12-22(16)34-26(38)20-9-18(14-32)10-21(11-20)39(27,28,29,30)31/h3-13,15H,1-2H3,(H,34,38)
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.{{Pazopanib} medchemexpress|{Pazopanib} VEGFR|{Pazopanib} Biological Activity|{Pazopanib} Description|{Pazopanib} custom synthesis|{Pazopanib} Autophagy}
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:
BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.|Product information|CAS Number: 1448316-08-2|Molecular Weight: 558.53|Formula: C26H19F5N6OS|Chemical Name: 3-cyano-N-{2,4-dimethyl-5-[6-(pyridin-3-yl)-1H-pyrazolo[1,5-a]imidazol-1-yl]phenyl}-5-(pentafluoro-λ⁶-sulfanyl)benzamide|Smiles: CC1C=C(C)C(=CC=1NC(=O)C1C=C(C=C(C=1)S(F)(F)(F)(F)F)C#N)N1C=CN2N=C(C=C21)C1=CN=CC=C1|InChiKey: MPASHPJAIUOWCK-UHFFFAOYSA-N|InChi: InChI=1S/C26H19F5N6OS/c1-16-8-17(2)24(36-6-7-37-25(36)13-23(35-37)19-4-3-5-33-15-19)12-22(16)34-26(38)20-9-18(14-32)10-21(11-20)39(27,28,29,30)31/h3-13,15H,1-2H3,(H,34,38)|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.|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:|BAY-826 is a selective and potent inhibitor of TIE-2 (dissociation constant = 1.{{D-Cycloserine} site|{D-Cycloserine} Anti-infection|{D-Cycloserine} Purity & Documentation|{D-Cycloserine} Formula|{D-Cycloserine} manufacturer|{D-Cycloserine} Epigenetics} 6 nM) and binds with similar high affinity to only 4 of 456 tested kinases, namely, TIE-1, DDR1, DDR2, and Serine/threonine-protein kinase 10 (LOK) (dissociation constant = 0.PMID:23399686 9, 0.4,1.3, and 5.9 nM).The high biochemical affinity for TIE-2 translates into very potent cellular mechanistic activity with an EC50 of about 1.3 nM for inhibition of TIE-2 autophosphorylation in human umbilical vein endothelial cells. The TIE-2 inhibitor BAY-826 is tested for its acute growth inhibitory as well as anti-clonogenic properties in all four mouse glioma cell lines. BAY-826 is highly selective against other angiogenic kinases, such as VEGFR, fibroblast growth factorreceptor (FGFR), or Platelet-derived growth factor receptor (PDGFR), and affects VEGF-stimulated proliferation of HUVEC only atμM concentrations, respectively.|In Vivo:|BAY-826 (oral gavage; 25 mg/kg,50 mg/kg,100 mg/k) potently inhibits ANG-1-stimulated TIE-2 autophosphorylation in murine lungs in female CB17/scid mice. BAY-826 improves tumor control in syngeneic mouse glioma models. Co-treatment with BAY-826 and irradiation is ineffective in one model (SMA-497), but provided synergistic prolongation of survival in another (SMA-560) cell. TIE- 2 inhibition may improve tumor response to treatment in highly vascularized tumors such as glioblastoma.|Products are for research use only. Not for human use.|