SML2498

Vatalanib dihydrochloride

≥98% (HPLC)

• Synonym(s): 1-(4-Chloroanilino)-4-(4-pyridylmethyl)phthalazine dihydrochloride, CGP 79787 dihydrochloride, CGP 79787D dihydrochloride, N-(4-Chloroanilino)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride, PTK 787 dihydrochloride, PTK787 dihydrochloride, ZK 222584 dihydrochloride, ZK-222584 dihydrochloride, ZK222584 dihydrochloride
• Empirical Formula (Hill Notation): C₂₀H₁₅ClN₄ · 2HCl
• CAS Number: 212141-51-0
• Molecular Weight: 419.73
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD08458963
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Properties

• 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

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable