产品介绍
Product Description
Biochem/physiol Actions
Orally active anti-angiogenic agent that targets receptor tyrosine kinases VEGFR1/2/3 (FLT-1/KDR/FLT-4), PDGFRβ, c-KIT and c-FMS.
Vatalanib (PTK787, ZK 222584, CGP 79787D, CGP 79787 succinate) is an orally active anilinophthalazine derivative that exerts its anti-angiogenic efficacy by targeting receptor tyrosine kinase (RTK) VEGFR (VEGFR1/2 IC50 = 54/39 nM; IC50 ∼30 nM against 100 ng/mL VEGF-C-induced VEGFR3 autophosphorylation in MEVCs) and, to a less extent, PDGFRβ, c-kit, c-fms (IC50 = 364, 600, 567 nM, respectively) in an ATP-competitive manner with much reduced or no potency toward >90 other kinases. Typical dosing ranges: 0.1-10 μM in cultures, 5 nM-200 μM (zebrafish) and 30-100 mg/kg (mice & rats via po. or ip) in vivo.
技术参数
Specifications
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | ClC(C=C1)=CC=C1NC2=NN=C(CC3=CC=NC=C3)C4=CC=CC=C42 |
| InChI | 1S/C20H15ClN4.2ClH/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14;;/h1-12H,13H2,(H,23,25);2*1H |
| InChI key | AZUQEHCMDUSRLH-UHFFFAOYSA-N |

