Vatalanib

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.

Product information

CAS Number: 212141-54-3

Molecular Weight: 346.81

Formula: C20H15ClN4

Synonym:

PTK787

PTK 787

PTK-787

ZK 222584

ZK222584

ZK-222584

CGP 79787

CGP-797870

ZK-232934

CGP79787D

PTK787/ZK 222584

CGP-7978

Related CAS Number:

212142-18-2 (Vatalanib succinate)

212141-51-0 (Vatalanib hydrochloride)

Chemical Name: N-(4-chlorophenyl)-4-[(pyridin-4-yl)methyl]phthalazin-1-amine

Smiles: ClC1C=CC(=CC=1)NC1=NN=C(CC2C=CN=CC=2)C2=CC=CC=C21

InChiKey: YCOYDOIWSSHVCK-UHFFFAOYSA-N

InChi: InChI=1S/C20H15ClN4/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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 85 mg/mLwarmed(202.51 mM). Water: 10 mg/mL(23.82 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.

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.

References:

1. Murakami M, et al. Ann Surg Oncol. 2011, 18(2), 589-596.
2. Wood JM, et al. Cancer Res. 2000, 60(8), 2178-2189.

Products are for research use only. Not for human use.