Bms582664
Brivanib Alaninate (BMS-582664)
CAS: 649735-63-7
Molecular Formula: C22H24FN5O4
Bms582664 - Names and Identifiers
Bms582664 - Physico-chemical Properties
| Molecular Formula | C22H24FN5O4 |
| Molar Mass | 441.46 |
| Density | 1.42±0.1 g/cm3(Predicted) |
| Solubility | DMSO 88 mg/mL Water <1 mg/mL Ethanol 88 mg/mL |
| Appearance | Yellow powder. |
| pKa | 16.08±0.30(Predicted) |
| Storage Condition | -20℃ |
| Use | Brivanib Alaninate (BMS-582664) is a BMS-540215 prodrug and an ATP competitive VEGFR2 inhibitor with an IC50 of 25 nM. |
| In vitro study | BMS-582664 inhibited VEGF and FGF-stimulated HUVECs proliferation with IC50 of 40 nM and 276 nM, respectively. BMS-582664 (2 μm) significantly inhibited the phosphorylation of SK-HEP1, HepG-2, ERK1/2 and Akt in VEGFR-2 and FGFR-1 cells stimulated by VEGF and bFGF, BMS-582664 alone had no effect on phosphorylation levels of ERK1/2, Akt, VEGFR-2, and FGFR-1 in unstimulated cells. BMS-582664 inhibits CYP2C19, CYP3A4(BFC) and CYP3A4 (BzRes) with IC50 of 2.4 μm, 0.51 μm and 1.6 μm, respectively. BMS-582664 has high solid-state stability (only 0.3% degradation at 50°C during 12 weeks of desiccant placement) and considerable liquid-state stability at pH 6.5. |
| In vivo study | Mice were treated with BMS-582664 (50 mg/kg) with an AUC of 136 μm×hr and a Cmax of 41 μm. BMS-582664 (60 mg/kg, oral) treated mice, rapidly absorbed, T max of 1 hour, half-life (t 1/2) of 2.7 hours, mean residence time (MRT) 3.6 hours. BMS-582664 Rats (25 mg/kg) were treated with an AUC of 13.4 μm×hr and a Cmax of 6.4 μm. Treatment of athymic mice carrying H3396 tumor xenografts BMS-582664 inhibited tumor growth by 85% and 97% at 60 mg/kg and 90 mg/kg, respectively, this effect was dose-dependent. Treatment of mice carrying patient-derived xenografts 06-0606 at doses of 50 mg/kg and 100 mg/kg BMS-582664 inhibited tumor growth by 55% and 13%, respectively. BMS-582664(60 mg/kg, oral) in mice carrying patient-derived transplanted tumor 06-0606, significantly reduced tumor weight, promoted apoptosis, reduced microvessel density, inhibited cell proliferation, and down regulation of cell cycle. Treatment of non-thymic mice carrying L2987 non-small cell lung cancer xenografts BMS-582664 inhibited tumor growth by 107 and 85% at doses of 80 mg/kg and 97% mg/kg, respectively, this effect was dose-dependent. BMS-582664 (100 mg/kg) inhibited new growth of vascular endothelial cells in two xenograft-bearing mouse models, L2987 and hct116. |
Bms582664 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.265 ml | 11.326 ml | 22.652 ml |
| 5 mM | 0.453 ml | 2.265 ml | 4.53 ml |
| 10 mM | 0.227 ml | 1.133 ml | 2.265 ml |
| 5 mM | 0.045 ml | 0.227 ml | 0.453 ml |
Last Update：2024-01-02 23:10:35
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View History
Bms582664
奥司他韦杂质F盐酸盐
Benzothiazole, 2-[[2-(phenylmethoxy)ethyl]thio]-
Trisodium Hydrogen Ethylenediaminetetraacetate Hydrate [for Biochemical Research]
140911-22-4
benzoyl chloride, 2-[(3,4-dichlorophenyl)methoxy]-3-methox
1-VINYL-1 H-PYRROLE-2-CARBOXYLIC ACID
3-METHOXYPENYLBORONIC ACID
4-TERT-BUTYLPHENYL ISOTHIOCYANATE
N-METHYL 4-FLUOROBENZENESULFONAMIDE
奥司他韦杂质F盐酸盐
Benzothiazole, 2-[[2-(phenylmethoxy)ethyl]thio]-
Trisodium Hydrogen Ethylenediaminetetraacetate Hydrate [for Biochemical Research]
140911-22-4
benzoyl chloride, 2-[(3,4-dichlorophenyl)methoxy]-3-methox
1-VINYL-1 H-PYRROLE-2-CARBOXYLIC ACID
3-METHOXYPENYLBORONIC ACID
4-TERT-BUTYLPHENYL ISOTHIOCYANATE
N-METHYL 4-FLUOROBENZENESULFONAMIDE