BAY-826
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
Size | Price | Stock |
---|---|---|
100mg | $1650 | To Be Confirmed |
250mg | $2650 | To Be Confirmed |
500mg | $3975 | To Be Confirmed |
Cat #: V4169 CAS #: 1448316-08-2 Purity ≥ 98%
Description: BAY-826 is a novel, highly potent, selective and orally available small molecule TIE-2 inhibitor with Kd of 1.6 nM, respectively.
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Molecular Weight (MW) | 558.53 |
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Molecular Formula | C26H19F5N6OS |
CAS No. | 1448316-08-2 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
SMILES Code | O=C(NC1=CC(N2C=CN3N=C(C4=CC=CN=C4)C=C32)=C(C)C=C1C)C5=CC(S(F)(F)(F)(F)F)=CC(C#N)=C5 |
Synonyms | BAY826; BAY 826; BAY-826 |
Protocol | In Vitro | BAY-826 is a selective and potent inhibitor of TIE-2 (dissociation constant = 1.6 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 = 0.9, 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. |
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In Vivo | 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. 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7904 mL | 8.9521 mL | 17.9041 mL | 35.8083 mL |
5mM | 0.3581 mL | 1.7904 mL | 3.5808 mL | 7.1617 mL |
10mM | 0.1790 mL | 0.8952 mL | 1.7904 mL | 3.5808 mL |
20mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 1.7904 mL |
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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