Avapritinib
作者：齐岳
发布时间：2023-08-28
09:02:40
点击数：
产品名称：Avapritinib
产品描述：
| 产品描述 | Avapritinib is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM). |
| 靶点活性 | KIT D816V:0.27 nM, PDGFRα D842V:0.24 nM |
| 体外活性 | Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, at positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50: 40 nM), downstream signaling, as well as cellular proliferation (IC50: 75 nM)[1]. |
| 体内活性 | BLU-285 (0.3-30 mg/kg) reduces tumor volume in a P815 KITD814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies. |
| 动物实验 | A Kasumi-1 luc+ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post-injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45. Control groups are treated with vehicle or Cytarabine administered 100 mg/kg i.p once weekly. |
| 别名 | BLU-285 |
| 分子量 | 498.57 |
| 分子式 | C26H27FN10 |
| CAS No. | 1703793-34-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: Insoluble
Ethanol: 3 mg/mL
DMSO: 65 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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