Identification | Back Directory | [Name]
BAY-826
(BAY826) | [CAS]
1448316-08-2 | [Synonyms]
BAY-826
(BAY826) [3-Cyano-5-[[[2,4-dimethyl-5-[6-(3-pyridinyl)-1H-imidazo[1,2-b]pyrazol-1-yl]phenyl]amino]carbonyl]phenyl]pentafluorosulfur | [Molecular Formula]
C26H19F5N6OS | [MDL Number]
MFCD31657322 | [MOL File]
1448316-08-2.mol | [Molecular Weight]
558.53 |
Hazard Information | Back Directory | [Description]
BAY-826 is a highly potent, orally available TIE-2-inhibitor which improves tumor control in syngeneic mouse glioma models. | [Uses]
BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively. | [Definition]
ChEBI: BAY-826 is a secondary carboxamide resulting from the formal condensation of the carboxy group of 3-cyano-5-(pentafluoro-lambda(6)-sulfanyl)benzoic acid with the amino group of 2,4-dimethyl-5-[6-(pyridin-3-yl)-1H-imidazo[1,2-b]pyrazol-1-yl]aniline. It is a potent TIE-2 inhibitor (Kd = 1.6 nM) which displays in vivo efficacy in some murine glioma models. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a member of pyridines, an imidazopyrazole, a member of benzamides, a secondary carboxamide, a nitrile, an organofluorine compound and an organosulfur compound. | [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[1].
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[1]. | [IC 50]
Tie2: 1.6 nM (Kd) | [storage]
Store at -20°C | [References]
[1] Schneider H, et al. J Neurochem. 2017 Jan; 140(1):170-182. doi: 10.1111/jnc.13877. Epub 2016 Dec 12.Novel TIE-2 inhibitor BAY-826 displays in vivo efficacy in experimental syngeneic murine glioma models. DOI:10.1111/jnc.13877 |
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Company Name: |
BOC Sciences
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Tel: |
1-631-485-4226; 16314854226 |
Website: |
https://www.bocsci.com |
Company Name: |
InvivoChem
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Tel: |
13549236410 |
Website: |
https://www.invivochem.cn/ |
Company Name: |
R&D Systems, Inc
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Tel: |
18003437475 18003437475 |
Website: |
www.rndsystems.com |
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