Erdafitinib
作者：齐岳
发布时间：2023-08-28
09:00:54
点击数：
产品名称：Erdafitinib
产品描述：
| 产品描述 | Erdafitinib is a quinoxaline derivative compound, acts on FGFR1/2/3/4. |
| 靶点活性 | FGFR4:5.7 nM, FGFR3:3.0nM, FGFR1:1.2 nM, FGFR2:2.5nM |
| 体外活性 | JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival[2]. |
| 体内活性 | In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control[2]. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components[1]. |
| 细胞实验 | The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2) and trypan blue dye exclusion for the suspension cells, NCI-H716. (Only for Reference) |
| 别名 | JNJ-42756493, 厄达替尼 |
| 分子量 | 446.555 |
| 分子式 | C25H30N6O2 |
| CAS No. | 1346242-81-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 15 mg/mL(33.6 mM)
H2O: <1 mg/mL
DMSO: 82 mg/mL (183.6 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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