Information Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of thetyrosine kinaseactivity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. Targets PDGFR (Cell-free assay); Flk-1/DFR (Cell-free asssay) 5 nM(Ki); 6 nM(Ki) In vitro Toceranib (SU11654) competes directly with ATP at the intracellular kinase domain of the RTK, thus preventing tyrosine phosphorylation and subsequent signal transduction. SU11654 exerts a potent antiproliferative effect on endothelial cells. Additionally, SU11654 treatment can induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in split kinase RTKs. In vivo In mouse xenograft models, oral administration of SU11654 and related compounds affects the growth of multiple tumor cell lines originating from a variety of tissues, leading to either tumor regression or tumor growth inhibition. Cell Research(from reference) Cell lines:BR, C2, and P815 cells Concentrations:0.01 to 1 μM Incubation Time:24, 48, and 72 hours
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Toceranib phosphate
Dangerous GoodsCAS number:874819-74-6 molecular formula:C22H25FN4O2.H3O4P
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Specs
| Chinese alias | 磷酸托西尼布 | ||
| English alias | 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide;phosphoric acid | SU11654 phosphate | 5-[(Z)-(5-Fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(pyrrolidin-1-yl)ethyl | ||
| CAS number | 874819-74-6 | molecular formula | C22H25FN4O2.H3O4P |
| molecular weight | 494.45 g/mol | Exact mass | ≥98% |
| PSA | 155.000 Ų | logp | 2.292 |
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Safety information
pictogram:
GHS08
Signal word:
Danger
Hazard Statement:
H372: 通过长时间或反复暴露对器官造成损害 H360: 可能损害生育力或未出生的孩子
Statement of Preventive Measures:
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P203: 使用前,获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心,请就医。 P319: 如果你感到不适,请寻求医疗帮助。
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