Vatalanib Dihydrochloride 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

Vatalanib Dihydrochloride 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

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

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.

in vivo

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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