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212141-51-0

212141-51-0 Structure

212141-51-0 Structure
IdentificationMore
[Name]

Vatalanib Dihydrochloride
[CAS]

212141-51-0
[Synonyms]

PTK/ZK
ZK-222584
CGP-79787
CGP-79787D
Vatalanib (PTK787) 2HCl
Vatalanib 2HCl (PTK787)
CGP-79787 Dihydrochlorid
Vatalanib Dihydrochloride
CGP-79787 Dihydrochloride
ZK 222584 (cpg-79787) 2HCl
CGP-79787, PTK 787, ZK222584
Vatalanib 2hcl((ZK-222584,PTK 787)
Vatalanib dihydrochloride (PTK787)
N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine Dihydrochloride
N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride
[Molecular Formula]

C20H17Cl3N4
[MDL Number]

MFCD08458964
[MOL File]

212141-51-0.mol
[Molecular Weight]

419.74
Chemical PropertiesBack Directory
[Appearance]

White to Off-White Crystalline Powder
[Melting point ]

268-2700C
[storage temp. ]

Refrigerator
[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.
[CAS DataBase Reference]

212141-51-0
Hazard InformationBack Directory
[Chemical Properties]

White to Off-White Crystalline Powder
[Usage]

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

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.
[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.
[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.
[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)
[storage]

Store at -20°C
[References]

1) Wood?et al. (2000),?PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration;? Cancer Res.,?60?2178 2) Lin?et al. (2002),?The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in bone marrow microenvironment;? Cancer Res.,?62?5019
Safety DataBack Directory
[Risk Statements ]

36/37/38
[Safety Statements ]

24/25
[HS Code ]

29333990
Spectrum DetailBack Directory
[Spectrum Detail]

Vatalanib Dihydrochloride(212141-51-0)1HNMR
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