av-951
N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea
CAS: 475108-18-0
Molecular Formula: C22H19ClN4O5
av-951 - Names and Identifiers
| Name | N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea |
| Synonyms | CS-8 AV951 AV-951 av-951 KRN951 AV 951 Tivozanib EPERTINIB HCL, S-222611 HYDROCHLORIDE, S-222611 HCL AV951(KRN951, Tivozanib) (stopped use since the patent issue) N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea n-(2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-n'-(5-methyl-3-isoxazolyl)urea Tivozanib, AV951,N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea |
| CAS | 475108-18-0 |
av-951 - Physico-chemical Properties
| Molecular Formula | C22H19ClN4O5 |
| Molar Mass | 454.86 |
| Density | 1.421 |
| Melting Point | >202°C (dec.) |
| Boling Point | 550.4±50.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly, Heated) |
| Appearance | White powder. |
| Color | Pale Beige to Light Brown |
| pKa | 11.74±0.70(Predicted) |
| Storage Condition | Refrigerator |
| In vitro study | AV-951 also inhibited the phosphorylation of pdgfrß and c-Kit with an IC50 of 1.72nM and 1.63nM, respectively. AV-951 blocks VEGF-dependent MAPK activity and endothelial cell proliferation. AV-951 is a new type of Quinoline-urea derivatives. |
| In vivo study | In vivo studies have shown that AV-951 reduces the microvessel density of the transplanted tumor and inhibits the level of phosphorylation VEGFR-2 the transplanted tumor, especially when the AV-951 concentration is 1 mg/kg (oral treatment). In athymic mice, AV-951 inhibited almost all of the xenografts, with a tumor growth inhibition rate (TGI) of> 85%. AV-951 showed anticancer activity in human xenograft models including lung, thymus, colon, ovary, pancreas and prostate cancer. A murine peritoneal diffuse tumor model study has shown that AV-951 prolongs the life of tumor-bearing mice. |
av-951 - Reference Information
| biological activity | Tivozanib (AV-951) is an effective, selective VEGFR inhibitor. when acting on VEGFR1/2/3, IC50 is 0.21 nM/0.16 nM/0.24 nM respectively, which also inhibits PDGFR and c-Kit, acts on FGFR-1, Flt3, c-Met EGFR and IGF-1R activities are weak. Phase 3. Tivozanib (AV-951, KRN-951) is an effective and selective VEGFR inhibitor. when acting on VEGFR1/2/3, IC50 is 0.21 nM/0.16 nM/0.24 nM respectively. it also inhibits PDGFR and c-Kit. it acts on FGFR-1, Flt3, c-Met EGFR and IGF-1R activities are weak. Phase 3. |
| Target | Value |
| VEGFR2 (Cell-free assay) | 6.5 nM |
| VEGFR3 (Cell-free assay) | 15 nM |
| EphB2 (Cell-free assay) | 24 nM |
| VEGFR1 (Cell-free assay) | 30 nM |
| PDGFRα (Cell-free assay) | 40 nM |
Last Update：2024-04-09 15:16:50
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Spot supply
Product Name: Tivozanib Visit Supplier Webpage Request for quotationCAS: 475108-18-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Tivozanib (AV-951) Visit Supplier Webpage Request for quotationCAS: 475108-18-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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