Vatalanib 2HCl (212141-51-0) is a potent, selective inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50 = 77 nM) and VEGFR-2 (FLK-1/KDR, IC50 = 37 nM).1 Weaker inhibitor of other tyrosine kinases including PDGFR-β (IC50 = 580 nM), c-KIT (IC50 = 730 nM), FLT-4 (IC50 = 660 nM) and c-FMS (IC50 = 1.4 μM). Inactive against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC50 > 10 μM). Vatalanib 2HCl inhibits the growth of multiple myeloma cells in the bone marrow microenvironment.2 瓦他拉尼碱 2HCl(212141-51-0)是VEGFR酪氨酸激酶VEGFR-1 (Flt-1, IC50 = 77 nM)和VEGFR-2 (FLK-1/KDR, IC50 = 37 nM)的一种有效的选择性抑制剂 对其他酪氨酸激酶PDGFR-β (IC50 = 580 nM)、c-KIT (IC50 = 730 nM)、FLT-4 (IC50 = 660 nM)和c-FMS (IC50 = 1.4 μM)的抑制作用较弱。 对EGFR、c-SRC、v-ABL和蛋白激酶Cα无活性(IC50 > 10 μM)。 Vatalanib 2HCl在骨髓微环境中抑制多发性骨髓瘤细胞生长
References/Citations:
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., 62 501
CAS:
212141-51-0
Catalog Number:
10-2183
Activity:
VEGFRK inhibitor
Chemical Name:
N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine dihydrochloride
Alternate Names:
CGP-79787; PTK-787; ZK222584
Molecular Weight:
419.73
Molecular Formula:
C20H15ClN4 &bul; 2HCl
Solubility:
Soluble in DMSO (up to 20 mg/ml with warming) or in Water (up to 100 mg/ml)
Physical Properties:
White or off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT
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