ChemicalBook Product Catalog Biochemical Engineering Inhibitors protein tyrosine kinase Vatalanib Dihydrochloride

Vatalanib Dihydrochloride

Product NameVatalanib Dihydrochloride
CAS212141-51-0
MFC20H17Cl3N4
MW419.74
EINECS
MOL File212141-51-0.mol

Chemical Properties

Melting point	268-2700C
storage temp.	Inert atmosphere,Store in freezer, under -20°C
solubility	Soluble in DMSO (up to 20 mg/ml with warming) or in Water (up to 100 mg/ml)
form	solid
color	White or off-white
Water Solubility	H2O: 2mg/mL, clear
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
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
InChIKey	AZUQEHCMDUSRLH-UHFFFAOYSA-N
SMILES	ClC(C=C1)=CC=C1NC2=NN=C(CC3=CC=NC=C3)C4=CC=CC=C42
CAS DataBase Reference	212141-51-0

Safety Information

Risk Statements	36/37/38
Safety Statements	24/25
WGK Germany	WGK 3
HS Code	29333990
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC₅₀ values of 77, 37, and 190 nM, respectively. It less potently inhibits PDGF and c-Kit (IC₅₀ = 600 and 700 nM) and has no effect on a large panel of additional kinases. Vatalanib completely blocks retinal neovascularization in oxygen-induced ischemic retinopathy in mice, suggesting its use in diabetic retinopathy and other diseases featuring aberrant vascular development.

Chemical Properties

White to Off-White Crystalline Powder

Uses

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR, Flt-1 and c-Kit with IC50 of 37 nM, 77 nM and 730 nM, respectively.

Uses

Vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor. Antineoplastic.

in vivo

Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes^[1].

IC 50

VEGFR2: 37 nM (IC₅₀)

References

[1] J M WOOD. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.[J]. Cancer research, 2000, 60 8: 2178-2189.
[2] ANDERSON K. The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in the bone marrow microenvironment[J]. European Journal of Haematology, 2008, 70 4: 266-267. DOI:10.1034/j.1600-0609.2003.t01-1-01067.x

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